Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 37, Issue 1 (2022)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 37, Issue 1 (2022)

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Research Paper

Article
Dithiocarbamates effectively inhibit the α-carbonic anhydrase from Neisseria gonorrhoeae
Simone Giovannuzzi, Nader S. Abutaleb, Chad S. Hewitt, Fabrizio Carta, Alessio Nocentini, Mohamed N. Seleem, Daniel P. Flaherty & Claudiu T. Supuran
Pages: 1-8
Published online: 11 Dec 2021
AbstractforDithiocarbamates effectively inhibit the α-carbonic anhydrase from Neisseria gonorrhoeae | Full Text | References | PDF (2.7 MB)
  • 1688 Views
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Review

Review
A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors
Wenjing Liu, Min He, Yongjun Li, Zhiyun Peng & Guangcheng Wang
Pages: 9-38
Published online: 11 Dec 2021
AbstractforA review on synthetic chalcone derivatives as tubulin polymerisation inhibitors | Full Text | References | PDF (7.6 MB) | EPUB
  • 4254 Views
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Brief Report

Brief Report
Natural inspired piperine-based ureas and amides as novel antitumor agents towards breast cancer
Diaaeldin M. Elimam, Abdullah A. Elgazar, Fardous F. El-Senduny, Ramadan A. El-Domany, Farid A Badria & Wagdy M. Eldehna
Pages: 39-50
Published online: 11 Dec 2021
AbstractforNatural inspired piperine-based ureas and amides as novel antitumor agents towards breast cancer | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 3247 Views
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Research Papers

Article
Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of Neisseria gonorrhoeae
Nader S. Abutaleb, Ahmed E. M. Elhassanny, Alessio Nocentini, Chad S. Hewitt, Ahmed Elkashif, Bruce R. Cooper, Claudiu T. Supuran, Mohamed N. Seleem & Daniel P. Flaherty
Pages: 51-61
Published online: 11 Dec 2021
AbstractforRepurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of Neisseria gonorrhoeae | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 2715 Views
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Open Access
Article
Heterologous expression and biochemical characterisation of the recombinant β-carbonic anhydrase (MpaCA) from the warm-blooded vertebrate pathogen malassezia pachydermatis
Viviana De Luca, Andrea Angeli, Valeria Mazzone, Claudia Adelfio, Vincenzo Carginale, Andrea Scaloni, Fabrizio Carta, Silvia Selleri, Claudiu T. Supuran & Clemente Capasso
Pages: 62-68
Published online: 11 Dec 2021
AbstractforHeterologous expression and biochemical characterisation of the recombinant β-carbonic anhydrase (MpaCA) from the warm-blooded vertebrate pathogen malassezia pachydermatis | Full Text | References | PDF (1.7 MB) | EPUB
  • 1658 Views
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Open Access
Article
Design, synthesis, and evaluation of chalcone-Vitamin E-donepezil hybrids as multi-target-directed ligands for the treatment of Alzheimer’s disease
Zhipei Sang, Qing Song, Zhongcheng Cao, Yong Deng & Li Zhang
Pages: 69-85
Published online: 11 Dec 2021
AbstractforDesign, synthesis, and evaluation of chalcone-Vitamin E-donepezil hybrids as multi-target-directed ligands for the treatment of Alzheimer’s disease | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 3048 Views
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Open Access
Article
Novel sulphonamide-bearing methoxyquinazolinone derivatives as anticancer and apoptosis inducers: synthesis, biological evaluation and in silico studies
Ali S. Alqahtani, Mostafa M. Ghorab, Fahd A. Nasr, Mohammad Z. Ahmed, Abdullah A. Al-Mishari & Sabry M. Attia
Pages: 86-99
Published online: 11 Dec 2021
AbstractforNovel sulphonamide-bearing methoxyquinazolinone derivatives as anticancer and apoptosis inducers: synthesis, biological evaluation and in silico studies | Full Text | References | PDF (2.7 MB) | EPUB
  • 2355 Views
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Article
Mechanism of biotin carboxylase inhibition by ethyl 4-[[2-chloro-5-(phenylcarbamoyl)phenyl]sulphonylamino]benzoate
Matthew K. Craft & Grover L. Waldrop
Pages: 100-108
Published online: 11 Dec 2021
AbstractforMechanism of biotin carboxylase inhibition by ethyl 4-[[2-chloro-5-(phenylcarbamoyl)phenyl]sulphonylamino]benzoate | Full Text | References | PDF (1.7 MB) | EPUB
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Article
Discovery of a novel Aurora B inhibitor GSK650394 with potent anticancer and anti-aspergillus fumigatus dual efficacies in vitro
Yuhua He, Wei Fu, Liyang Du, Huiqiao Yao, Zhengkang Hua, Jinyu Li & Zhonghui Lin
Pages: 109-117
Published online: 11 Dec 2021
AbstractforDiscovery of a novel Aurora B inhibitor GSK650394 with potent anticancer and anti-aspergillus fumigatus dual efficacies in vitro | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Article
Dasatinib ameliorates thioacetamide-induced liver fibrosis: modulation of miR-378 and miR-17 and their linked Wnt/β-catenin and TGF-β/smads pathways
Mai A. Zaafan & Amr M. Abdelhamid
Pages: 118-124
Published online: 11 Dec 2021
AbstractforDasatinib ameliorates thioacetamide-induced liver fibrosis: modulation of miR-378 and miR-17 and their linked Wnt/β-catenin and TGF-β/smads pathways | Full Text | References | PDF (2.5 MB) | EPUB
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Article
The discovery of a novel series of potential ERRα inverse agonists based on p-nitrobenzenesulfonamide template for triple-negative breast cancer in vivo
Zhipei Gao, Tianxiao Wang, Rui Li, Yongli Du, Han Lv, Liudi Zhang, Haifei Chen, Xiaojin Shi, Qunyi Li & Jingkang Shen
Pages: 125-134
Published online: 11 Dec 2021
AbstractforThe discovery of a novel series of potential ERRα inverse agonists based on p-nitrobenzenesulfonamide template for triple-negative breast cancer in vivo | Full Text | References | PDF (2.2 MB) | EPUB
  • 2032 Views
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Article
Ultrasound promoted green synthesis, anticancer evaluation, and molecular docking studies of hydrazines: a pilot trial
Amena Ali, Abuzer Ali, Abu Tahir, Mohammed Afroz Bakht & Mohamed Jawed Ahsan
Pages: 135-144
Published online: 11 Dec 2021
AbstractforUltrasound promoted green synthesis, anticancer evaluation, and molecular docking studies of hydrazines: a pilot trial | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 1851 Views
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Brief Reports

Brief Report
New PIN1 inhibitors identified through a pharmacophore-driven, hierarchical consensus docking strategy
Giulio Poli, Miriana Di Stefano, Joan Arias Estevez, Filippo Minutolo, Carlotta Granchi, Antonio Giordano, Salvatore Parisi, Matteo Mauceri, Vincenzo Canzonieri, Marco Macchia, Isabella Caligiuri, Tiziano Tuccinardi & Flavio Rizzolio
Pages: 145-150
Published online: 11 Dec 2021
AbstractforNew PIN1 inhibitors identified through a pharmacophore-driven, hierarchical consensus docking strategy | Full Text | References | PDF (1.4 MB) | EPUB
  • 2675 Views
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Article
Novel 3-chloro-6-nitro-1H-indazole derivatives as promising antileishmanial candidates: synthesis, biological activity, and molecular modelling studies
Mohamed Mokhtar Mohamed Abdelahi, Youness El Bakri, Chin-Hung Lai, Karthikeyan Subramani, El Hassane Anouar, Sajjad Ahmad, Mohammed Benchidmi, Joel T. Mague, Jelena Popović-Djordjević & Souraya Goumri-Said
Pages: 151-167
Published online: 11 Dec 2021
AbstractforNovel 3-chloro-6-nitro-1H-indazole derivatives as promising antileishmanial candidates: synthesis, biological activity, and molecular modelling studies | Full Text | References | PDF (3.9 MB) | EPUB | Supplemental
  • 2395 Views
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Open Access
Article
2-Aminobenzoxazole-appended coumarins as potent and selective inhibitors of tumour-associated carbonic anhydrases
Alma Fuentes-Aguilar, Penélope Merino-Montiel, Sara Montiel-Smith, Socorro Meza-Reyes, José Luis Vega-Báez, Adrián Puerta, Miguel X. Fernandes, José M. Padrón, Andrea Petreni, Alessio Nocentini, Claudiu T. Supuran, Óscar López & José G. Fernández-Bolaños
Pages: 168-177
Published online: 11 Dec 2021
Abstractfor2-Aminobenzoxazole-appended coumarins as potent and selective inhibitors of tumour-associated carbonic anhydrases | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 1742 Views
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Brief Report

Brief Report
Discovery of caffeoylisocitric acid as a Keap1-dependent Nrf2 activator and its effects in mesangial cells under high glucose
Huankai Yao, Wenting Zhang, Feng Yang, Fengwei Ai, Dan Du & Yan Li
Pages: 178-188
Published online: 11 Dec 2021
AbstractforDiscovery of caffeoylisocitric acid as a Keap1-dependent Nrf2 activator and its effects in mesangial cells under high glucose | Full Text | References | PDF (2.6 MB) | EPUB
  • 2168 Views
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Research Papers

Article
Synthesis and biological evaluation of halogenated phenoxychalcones and their corresponding pyrazolines as cytotoxic agents in human breast cancer
Peter A. Halim, Rasha A. Hassan, Khaled O. Mohamed, Soha O. Hassanin, Mona G. Khalil, Amr M. Abdou & Eman O. Osman
Pages: 189-201
Published online: 11 Dec 2021
AbstractforSynthesis and biological evaluation of halogenated phenoxychalcones and their corresponding pyrazolines as cytotoxic agents in human breast cancer | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
  • 2369 Views
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Open Access
Article
A polypeptide inhibitor of calcineurin blocks the calcineurin-NFAT signalling pathway in vivo and in vitro
Ping Wang, Wenying Li, Yumeng Yang, Na Cheng, Yuchen Zhang, Nan Zhang, Yanxia Yin, Li Tong, Zhimei Li & Jing Luo
Pages: 202-210
Published online: 11 Dec 2021
AbstractforA polypeptide inhibitor of calcineurin blocks the calcineurin-NFAT signalling pathway in vivo and in vitro | Full Text | References | PDF (1.7 MB) | EPUB
  • 1805 Views
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Article
New 1,2,4-oxadiazole derivatives with positive mGlu4 receptor modulation activity and antipsychotic-like properties
Anna Stankiewicz, Katarzyna Kaczorowska, Ryszard Bugno, Aneta Kozioł, Maria H. Paluchowska, Grzegorz Burnat, Barbara Chruścicka, Paulina Chorobik, Piotr Brański, Joanna M. Wierońska, Beata Duszyńska, Andrzej Pilc & Andrzej J. Bojarski
Pages: 211-225
Published online: 11 Dec 2021
AbstractforNew 1,2,4-oxadiazole derivatives with positive mGlu4 receptor modulation activity and antipsychotic-like properties | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 1703 Views
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Article
Structure-based virtual screening and biological evaluation of novel small-molecule BTK inhibitors
Tony Eight Lin, Li-Chin Sung, Min-Wu Chao, Min Li, Jia-Huei Zheng, Tzu-Ying Sung, Jui-Hua Hsieh, Chia-Ron Yang, Hsueh-Yun Lee, Er-Chieh Cho & Kai-Cheng Hsu
Pages: 226-235
Published online: 11 Dec 2021
AbstractforStructure-based virtual screening and biological evaluation of novel small-molecule BTK inhibitors | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 2555 Views
  • 1 CrossRef citations
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Open Access
Article
Synthesis and biological evaluation of celastrol derivatives as potent antitumor agents with STAT3 inhibition
Shaohua Xu, Ruolan Fan, Lu Wang, Weishen He, Haixia Ge, Hailan Chen, Wen Xu, Jian Zhang, Wei Xu, Yaqian Feng & Zhimin Fan
Pages: 236-251
Published online: 11 Dec 2021
AbstractforSynthesis and biological evaluation of celastrol derivatives as potent antitumor agents with STAT3 inhibition | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 3216 Views
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Open Access
Article
Polycyclic nitrogen heterocycles as potential thymidine phosphorylase inhibitors: synthesis, biological evaluation, and molecular docking study
Karen Aknin, Alexis Bontemps, Amaury Farce, Eric Merlet, Philippe Belmont, Philippe Helissey, Philippe Chavatte, Marie-Agnès Sari, Sylviane Giorgi-Renault & Stéphanie Desbène-Finck
Pages: 252-268
Published online: 22 Dec 2021
AbstractforPolycyclic nitrogen heterocycles as potential thymidine phosphorylase inhibitors: synthesis, biological evaluation, and molecular docking study | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 1900 Views
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Open Access
Article
TNP and its analogs: Modulation of IP6K and CYP3A4 inhibition
Seulgi Lee, Bernie Byeonghoon Park, Hongmok Kwon, Vitchan Kim, Jang Su Jeon, Rowoon Lee, Milan Subedi, Taehyeong Lim, Hyunsoo Ha, Dongju An, Jaehoon Kim, Donghak Kim, Sang Kyum Kim, Seyun Kim & Youngjoo Byun
Pages: 269-279
Published online: 11 Dec 2021
AbstractforTNP and its analogs: Modulation of IP6K and CYP3A4 inhibition | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
  • 1865 Views
  • 3 CrossRef citations
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Open Access
Article
Antiproliferative effects of sulphonamide carbonic anhydrase inhibitors C18, SLC-0111 and acetazolamide on bladder, glioblastoma and pancreatic cancer cell lines
Silvia Mussi, Sara Rezzola, Paola Chiodelli, Alessio Nocentini, Claudiu T. Supuran & Roberto Ronca
Pages: 280-286
Published online: 11 Dec 2021
AbstractforAntiproliferative effects of sulphonamide carbonic anhydrase inhibitors C18, SLC-0111 and acetazolamide on bladder, glioblastoma and pancreatic cancer cell lines | Full Text | References | PDF (1.5 MB) | EPUB
  • 2700 Views
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Article
Searching for drug leads targeted to the hydrophobic cleft of dengue virus capsid protein
Liliane O. Ortlieb, Ícaro P. Caruso, Nathane C. Mebus-Antunes, Andrea T. Da Poian, Elaine da C. Petronilho, José Daniel Figueroa-Villar, Claudia J. Nascimento & Fabio C. L. Almeida
Pages: 287-298
Published online: 11 Dec 2021
AbstractforSearching for drug leads targeted to the hydrophobic cleft of dengue virus capsid protein | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 1648 Views
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Article
Topo II inhibition and DNA intercalation by new phthalazine-based derivatives as potent anticancer agents: design, synthesis, anti-proliferative, docking, and in vivo studies
Mohamed M. Khalifa, Ahmed A. Al-Karmalawy, Eslam B. Elkaeed, Mohamed S. Nafie, Mohamed A. Tantawy, Ibrahim H. Eissa & Hazem A. Mahdy
Pages: 299-314
Published online: 11 Dec 2021
AbstractforTopo II inhibition and DNA intercalation by new phthalazine-based derivatives as potent anticancer agents: design, synthesis, anti-proliferative, docking, and in vivo studies | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 2671 Views
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Article
Design, synthesis, and biological evaluation of new thieno[2,3-d] pyrimidine derivatives as targeted therapy for PI3K with molecular modelling study
Fatma M. Elmenier, Deena S. Lasheen & Khaled A. M. Abouzid
Pages: 315-332
Published online: 26 Dec 2021
AbstractforDesign, synthesis, and biological evaluation of new thieno[2,3-d] pyrimidine derivatives as targeted therapy for PI3K with molecular modelling study | Full Text | References | PDF (3.1 MB) | EPUB
  • 2767 Views
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Open Access
Article
Coumarins effectively inhibit bacterial α-carbonic anhydrases
Simone Giovannuzzi, Chad S. Hewitt, Alessio Nocentini, Clemente Capasso, Daniel P. Flaherty & Claudiu T. Supuran
Pages: 333-338
Published online: 03 Jan 2022
AbstractforCoumarins effectively inhibit bacterial α-carbonic anhydrases | Full Text | References | PDF (1.3 MB)
  • 2155 Views
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Article
Identification of novel non-toxic and anti-angiogenic α-fluorinated chalcones as potent colchicine binding site inhibitors
Moran Sun, Minghua Yuan, Yingying Kang, Jinling Qin, Yixin Zhang, Yongtao Duan, Longfei Wang & Yongfang Yao
Pages: 339-354
Published online: 03 Jan 2022
AbstractforIdentification of novel non-toxic and anti-angiogenic α-fluorinated chalcones as potent colchicine binding site inhibitors | Full Text | References | PDF (4.2 MB) | Supplemental
  • 2755 Views
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Article
2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights
Mostafa M. Elbadawi, Wagdy M. Eldehna, Amer Ali Abd El-Hafeez, Warda R. Somaa, Amgad Albohy, Sara T. Al-Rashood, Keli K. Agama, Eslam B. Elkaeed, Pradipta Ghosh, Yves Pommier & Manabu Abe
Pages: 355-378
Published online: 20 Dec 2021
Abstractfor2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
  • 3038 Views
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Brief Report

Brief Report
Second generation β-elemene nitric oxide derivatives with reasonable linkers: potential hybrids against malignant brain glioma
Renren Bai, Junlong Zhu, Ziqiang Bai, Qing Mao, Yingqian Zhang, Zi Hui, Xinyu Luo, Xiang-Yang Ye & Tian Xie
Pages: 379-385
Published online: 10 Jan 2022
AbstractforSecond generation β-elemene nitric oxide derivatives with reasonable linkers: potential hybrids against malignant brain glioma | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2517 Views
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Research Papers

Article
1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies
Mohamed Hagras, Marwa A. Saleh, Rogy R. Ezz Eldin, Abdelrahman A. Abuelkhir, Emad Gamil Khidr, Ahmed A. El-Husseiny, Hesham A. El-Mahdy, Eslam B. Elkaeed & Ibrahim H. Eissa
Pages: 386-402
Published online: 20 Dec 2021
Abstractfor1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies | Full Text | References | PDF (4.6 MB) | EPUB | Supplemental
  • 2273 Views
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Article
New benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and in silico studies
Hazem Elkady, Alaa Elwan, Hesham A. El-Mahdy, Ahmed S. Doghish, Ahmed Ismail, Mohammed S. Taghour, Eslam B. Elkaeed, Ibrahim H. Eissa, Mohammed A. Dahab, Hazem A. Mahdy & Mohamed M. Khalifa
Pages: 403-416
Published online: 27 Dec 2021
AbstractforNew benzoxazole derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative evaluation, flowcytometric analysis, and in silico studies | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 2954 Views
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Article
Design, synthesis, and biological evaluation of biotinylated colchicine derivatives as potential antitumor agents
Chao Wang, Yujing Zhang, Zeyu Wang, Yuelin Li, Qi Guan, Dongming Xing & Weige Zhang
Pages: 417-426
Published online: 16 Dec 2021
AbstractforDesign, synthesis, and biological evaluation of biotinylated colchicine derivatives as potential antitumor agents | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 2122 Views
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Article
Flavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach
Katarzyna Jakimiuk, Suat Sari, Robert Milewski, Claudiu T. Supuran, Didem Şöhretoğlu & Michał Tomczyk
Pages: 427-436
Published online: 20 Dec 2021
AbstractforFlavonoids as tyrosinase inhibitors in in silico and in vitro models: basic framework of SAR using a statistical modelling approach | Full Text | References | PDF (2.6 MB) | EPUB
  • 3351 Views
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Brief Report

Brief Report
Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity
Jianan Sun, Jiahui Mu, Shenglin Wang, Cai Jia, Dahong Li, Huiming Hua & Hao Cao
Pages: 437-450
Published online: 27 Dec 2021
AbstractforDesign and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Research Papers

Article
Synthesis and bioactivities evaluation of oleanolic acid oxime ester derivatives as α-glucosidase and α-amylase inhibitors
Xu-Yang Deng, Jun-Jie Ke, Ying-Ying Zheng, Dong-Li Li, Kun Zhang, Xi Zheng, Jing-Ying Wu, Zhuang Xiong, Pan-Pan Wu & Xue-Tao Xu
Pages: 451-461
Published online: 10 Jan 2022
AbstractforSynthesis and bioactivities evaluation of oleanolic acid oxime ester derivatives as α-glucosidase and α-amylase inhibitors | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 2962 Views
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Article
Design, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors
Lingyue Zhao, Qian Yang, Yiqun Tang, Qidong You & Xiaoke Guo
Pages: 462-471
Published online: 10 Jan 2022
AbstractforDesign, synthesis, and biological evaluation of arylmethylpiperidines as Kv1.5 potassium channel inhibitors | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 1577 Views
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Article
Rational design and synthesis of 2-(1H-indazol-6-yl)-1H-benzo[d]imidazole derivatives as inhibitors targeting FMS-like tyrosine kinase 3 (FLT3) and its mutants
Daseul Im, Joonhong Jun, Jihyun Baek, Haejin Kim, Dahyun Kang, Hyunah Bae, Hyunwook Cho & Jung-Mi Hah
Pages: 472-486
Published online: 23 Jan 2022
AbstractforRational design and synthesis of 2-(1H-indazol-6-yl)-1H-benzo[d]imidazole derivatives as inhibitors targeting FMS-like tyrosine kinase 3 (FLT3) and its mutants | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
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Review

Review
Pharmaceutical strategies for preventing toxicity and promoting antioxidant and anti-inflammatory actions of bilirubin
Alessio Nocentini, Alessandro Bonardi, Simone Pratesi, Paola Gratteri, Carlo Dani & Claudiu T. Supuran
Pages: 487-501
Published online: 05 Jan 2022
AbstractforPharmaceutical strategies for preventing toxicity and promoting antioxidant and anti-inflammatory actions of bilirubin | Full Text | References | PDF (2.6 MB) | EPUB
  • 2971 Views
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Research Paper

Article
Synthesis, computational study and biological evaluation of 9-acridinyl and 1-coumarinyl-1,2,3-triazole-4-yl derivatives as topoisomerase II inhibitors
Gehan A. Abdel-Hafez, Abdel-Maaboud I. Mohamed, Adel F. Youssef, Claire Simons & Ahmed S. Aboraia
Pages: 502-513
Published online: 10 Jan 2022
AbstractforSynthesis, computational study and biological evaluation of 9-acridinyl and 1-coumarinyl-1,2,3-triazole-4-yl derivatives as topoisomerase II inhibitors | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Correction

Correction
Correction
Page: 514
Published online: 05 Jan 2022
CitationforCorrection | Full Text | PDF (89.4 KB) | EPUB
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Free Access

Research Paper

Article
Highly potent inhibitors of cathepsin K with a differently positioned cyanohydrazide warhead: structural analysis of binding mode to mature and zymogen-like enzymes
Jakub Benýšek, Michal Buša, Petra Rubešová, Jindřich Fanfrlík, Martin Lepšík, Jiří Brynda, Zuzana Matoušková, Ulrike Bartz, Martin Horn, Michael Gütschow & Michael Mareš
Pages: 515-526
Published online: 11 Feb 2022
AbstractforHighly potent inhibitors of cathepsin K with a differently positioned cyanohydrazide warhead: structural analysis of binding mode to mature and zymogen-like enzymes | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Brief Report

Brief Report
Replacing the phthalimide core in thalidomide with benzotriazole
Mikhail Krasavin, Andrey Bubyrev, Alexander Kazantsev, Christopher Heim, Samuel Maiwald, Daniil Zhukovsky, Dmitry Dar’in, Marcus D. Hartmann & Alexander Bunev
Pages: 527-530
Published online: 28 Feb 2022
AbstractforReplacing the phthalimide core in thalidomide with benzotriazole | Full Text | References | PDF (1.1 MB) | Supplemental
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Research Papers

Article
Discovery of 2,4-thiazolidinedione-tethered coumarins as novel selective inhibitors for carbonic anhydrase IX and XII isoforms
Wagdy M. Eldehna, Mohammed S. Taghour, Tarfah Al-Warhi, Alessio Nocentini, Mostafa M. Elbadawi, Hazem A. Mahdy, Mohamed A. Abdelrahman, Ohoud J. Alotaibi, Nada Aljaeed, Diaaeldin M. Elimam, Kamyar Afarinkia, Hatem A. Abdel-Aziz & Claudiu T. Supuran
Pages: 531-541
Published online: 07 Jan 2022
AbstractforDiscovery of 2,4-thiazolidinedione-tethered coumarins as novel selective inhibitors for carbonic anhydrase IX and XII isoforms | Full Text | References | PDF (1.7 MB) | Supplemental
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Article
Inhibitory effect of roburic acid in combination with docetaxel on human prostate cancer cells
Xiao Wang, Xu Xuetao, Mengshuo Wu, Panpan Wu, Zhaojun Sheng, Wenfeng Liu, Yan-Yan Ma, Den-Gao Zhao, Kun Zhang, Dongli Li, Xi Zheng & Susan Goodin
Pages: 542-553
Published online: 05 Jan 2022
AbstractforInhibitory effect of roburic acid in combination with docetaxel on human prostate cancer cells | Full Text | References | PDF (2.6 MB) | EPUB
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Article
In vitro α-glucosidase inhibition by Brazilian medicinal plant extracts characterised by ultra-high performance liquid chromatography coupled to mass spectrometry
Mariacaterina Lianza, Ferruccio Poli, Alan Menezes do Nascimento, Aline Soares da Silva, Thamirys Silva da Fonseca, Marcos Vinicius Toledo, Rosineide Costa Simas, Andréa Rodrigues Chaves, Gilda Guimarães Leitão & Suzana Guimarães Leitão
Pages: 554-562
Published online: 14 Feb 2022
AbstractforIn vitro α-glucosidase inhibition by Brazilian medicinal plant extracts characterised by ultra-high performance liquid chromatography coupled to mass spectrometry | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Article
Multi-stage structure-based virtual screening approach towards identification of potential SARS-CoV-2 NSP13 helicase inhibitors 
Mahmoud A. El Hassab, Wagdy M. Eldehna, Sara T. Al-Rashood, Amal Alharbi, Razan O. Eskandrani, Hamad M. Alkahtani, Eslam B. Elkaeed & Sahar M. Abou-Seri
Pages: 563-572
Published online: 10 Jan 2022
AbstractforMulti-stage structure-based virtual screening approach towards identification of potential SARS-CoV-2 NSP13 helicase inhibitors  | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 3346 Views
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Article
Synthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors
Abdallah E. Abdallah, Reda R. Mabrouk, Maged Mohammed Saleh Al Ward, Sally I. Eissa, Eslam B. Elkaeed, Ahmed B. M. Mehany, Mariam A. Abo-Saif, Ola A. El-Feky, Mohamed S. Alesawy & Mohamed Ayman El-Zahabi
Pages: 573-591
Published online: 10 Jan 2022
AbstractforSynthesis, biological evaluation, and molecular docking of new series of antitumor and apoptosis inducers designed as VEGFR-2 inhibitors | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
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Brief Report

Brief Report
First studies on tumor associated carbonic anhydrases IX and XII monoclonal antibodies conjugated to small molecule inhibitors
Chiara Testa, Anna Maria Papini, Reinhard Zeidler, Daniela Vullo, Fabrizio Carta, Claudiu T. Supuran & Paolo Rovero
Pages: 592-596
Published online: 20 Jan 2022
AbstractforFirst studies on tumor associated carbonic anhydrases IX and XII monoclonal antibodies conjugated to small molecule inhibitors | Full Text | References | PDF (1.2 MB) | EPUB
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Research Paper

Article
Regioselective approach to colchiceine tropolone ring functionalization at C(9) and C(10) yielding new anticancer hybrid derivatives containing heterocyclic structural motifs
Krystian Pyta, Natalia Skrzypczak, Piotr Ruszkowski, Franz Bartl & Piotr Przybylski
Pages: 597-605
Published online: 24 Jan 2022
AbstractforRegioselective approach to colchiceine tropolone ring functionalization at C(9) and C(10) yielding new anticancer hybrid derivatives containing heterocyclic structural motifs | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Reviews

Review
Glucokinase as an emerging anti-diabetes target and recent progress in the development of its agonists
Yixin Ren, Li Li, Li Wan, Yan Huang & Shuang Cao
Pages: 606-615
Published online: 24 Jan 2022
AbstractforGlucokinase as an emerging anti-diabetes target and recent progress in the development of its agonists | Full Text | References | PDF (1.6 MB) | EPUB
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Review
Research progress of coumarins and their derivatives in the treatment of diabetes
Yinbo Pan, Teng Liu, Xiaojing Wang & Jie Sun
Pages: 616-628
Published online: 24 Jan 2022
AbstractforResearch progress of coumarins and their derivatives in the treatment of diabetes | Full Text | References | PDF (1.8 MB) | EPUB
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Research Papers

Article
Discovery of triterpenoids as potent dual inhibitors of pancreatic lipase and human carboxylesterase 1
Jing Zhang, Qiu-Sha Pan, Xing-Kai Qian, Xiang-Lu Zhou, Ya-Jie Wang, Rong-Jing He, Le-Tian Wang, Yan-Ran Li, Hong Huo, Cheng-Gong Sun, Lei Sun, Li-Wei Zou & Ling Yang
Pages: 629-640
Published online: 31 Jan 2022
AbstractforDiscovery of triterpenoids as potent dual inhibitors of pancreatic lipase and human carboxylesterase 1 | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Article
Synthesis and evaluation of novel 1-(((6-substitutedbenzo[d]thiazol-2-yl)amino)(heteroaryl)methyl)naphthalen-2-ol as pesticidal agents
Junfeng Shang, Yuxin Li, Na Yang, Lixia Xiong & Baolei Wang
Pages: 641-651
Published online: 27 Jan 2022
AbstractforSynthesis and evaluation of novel 1-(((6-substitutedbenzo[d]thiazol-2-yl)amino)(heteroaryl)methyl)naphthalen-2-ol as pesticidal agents | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 1795 Views
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Article
Angiogenesis and anti-leukaemia activity of novel indole derivatives as potent colchicine binding site inhibitors
Yongfang Yao, Tao Huang, Yuyang Wang, Longfei Wang, Siqi Feng, Weyland Cheng, Longhua Yang & Yongtao Duan
Pages: 652-665
Published online: 02 Feb 2022
AbstractforAngiogenesis and anti-leukaemia activity of novel indole derivatives as potent colchicine binding site inhibitors | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
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Brief Reports

Brief Report
Inhibition studies of bacterial α-carbonic anhydrases with phenols
Simone Giovannuzzi, Chad S. Hewitt, Alessio Nocentini, Clemente Capasso, Gabriele Costantino, Daniel P. Flaherty & Claudiu T. Supuran
Pages: 666-671
Published online: 09 Feb 2022
AbstractforInhibition studies of bacterial α-carbonic anhydrases with phenols | Full Text | References | PDF (2 MB)
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Brief Report
Acipimox inhibits human carbonic anhydrases
Mattia Mori & Claudiu T. Supuran
Pages: 672-679
Published online: 09 Feb 2022
AbstractforAcipimox inhibits human carbonic anhydrases | Full Text | References | PDF (2.4 MB)
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Research Papers

Article
Coumarins inhibit η-class carbonic anhydrase from Plasmodium falciparum
Simone Giovannuzzi, Viviana De Luca, Alessio Nocentini, Clemente Capasso & Claudiu T. Supuran
Pages: 680-685
Published online: 09 Feb 2022
AbstractforCoumarins inhibit η-class carbonic anhydrase from Plasmodium falciparum | Full Text | References | PDF (1.7 MB)
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Article
Development of newly synthesised quinazolinone-based CDK2 inhibitors with potent efficacy against melanoma
Eman R. Mohammed & Ghada F. Elmasry
Pages: 686-700
Published online: 09 Feb 2022
AbstractforDevelopment of newly synthesised quinazolinone-based CDK2 inhibitors with potent efficacy against melanoma | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
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Article
Synthesis, molecular modelling and QSAR study of new N-phenylacetamide-2-oxoindole benzensulfonamide conjugates as carbonic anhydrase inhibitors with antiproliferative activity
Mona F. Said, Riham F. George, Andrea Petreni, Claudiu T. Supuran & Nada M. Mohamed
Pages: 701-717
Published online: 15 Feb 2022
AbstractforSynthesis, molecular modelling and QSAR study of new N-phenylacetamide-2-oxoindole benzensulfonamide conjugates as carbonic anhydrase inhibitors with antiproliferative activity | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Article
Comparative chemical and biological hydrolytic stability of homologous esters and isosteres
Hygor M. R. de Souza, Jéssica S. Guedes, Rosana H. C. N. Freitas, Luis G. V. Gelves, Harold H. Fokoue, Carlos Mauricio R. Sant’Anna, Eliezer J. Barreiro & Lidia M. Lima
Pages: 718-727
Published online: 13 Feb 2022
AbstractforComparative chemical and biological hydrolytic stability of homologous esters and isosteres | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2387 Views
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Article
Short divalent ethacrynic amides as pro-inhibitors of glutathione S-transferase isozyme Mu and potent sensitisers of cisplatin-resistant ovarian cancers
Bangtian Xu, Tingting Tong, Xin Wang, Fang Liu, Xiang Zhang, Xiaolei Hu, Xinpeng Li, Xiaolan Yang & Fei Liao
Pages: 728-742
Published online: 17 Feb 2022
AbstractforShort divalent ethacrynic amides as pro-inhibitors of glutathione S-transferase isozyme Mu and potent sensitisers of cisplatin-resistant ovarian cancers | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 1940 Views
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Brief Report

Brief Report
Isocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors
Mehmet Onyılmaz, Murat Koca, Alessandro Bonardi, Mustafa Degirmenci & Claudiu T. Supuran
Pages: 743-748
Published online: 21 Feb 2022
AbstractforIsocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors | Full Text | References | PDF (868.8 KB)
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Review

Review
Antibacterial action mechanisms and mode of trypsin inhibitors: a systematic review
Amanda Maria de Souza Nascimento, Victor Hugo de Oliveira Segundo, Ana Júlia Felipe Camelo Aguiar, Grasiela Piuvezam, Thaís Souza Passos, Karla Suzanne Florentino da Silva Florentino da Silva Chaves Damasceno & Ana Heloneida de Araújo Morais
Pages: 749-759
Published online: 16 Feb 2022
AbstractforAntibacterial action mechanisms and mode of trypsin inhibitors: a systematic review | Full Text | References | PDF (1.6 MB) | EPUB
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Research Papers

Article
Charged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides
Zuzana Kohoutova, David Malinak, Rudolf Andrys, Jana Svobodova, Miroslav Psotka, Monika Schmidt, Lukas Prchal & Kamil Musilek
Pages: 760-767
Published online: 23 Feb 2022
AbstractforCharged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1275 Views
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Article
Positional scanning of natural product hispidol’s ring-B: discovery of highly selective human monoamine oxidase-B inhibitor analogues downregulating neuroinflammation for management of neurodegenerative diseases
Ahmed H. E. Hassan, Hyeon Jeong Kim, Min Sung Gee, Jong-Hyun Park, Hye Rim Jeon, Cheol Jung Lee, Yeonwoo Choi, Suyeon Moon, Danbi Lee, Jong Kil Lee, Ki Duk Park & Yong Sup Lee
Pages: 768-780
Published online: 23 Feb 2022
AbstractforPositional scanning of natural product hispidol’s ring-B: discovery of highly selective human monoamine oxidase-B inhibitor analogues downregulating neuroinflammation for management of neurodegenerative diseases | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Brief Report

Brief Report
Thio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis
Alexandra Ibáñez-Escribano, Cristina Fonseca-Berzal, Mónica Martínez-Montiel, Manuel Álvarez-Márquez, María Gómez-Núñez, Manuel Lacueva-Arnedo, Teresa Espinosa-Buitrago, Tania Martín-Pérez, José Antonio Escario, Penélope Merino-Montiel, Sara Montiel-Smith, Alicia Gómez-Barrio, Óscar López & José G. Fernández-Bolaños
Pages: 781-791
Published online: 23 Feb 2022
AbstractforThio- and selenosemicarbazones as antiprotozoal agents against Trypanosoma cruzi and Trichomonas vaginalis | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1994 Views
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Research Paper

Article
Development of naringenin-O-alkylamine derivatives as multifunctional agents for the treatment of Alzheimer’s disease
Jing Yang, Yi Zhou, Yujuan Ban, Jing Mi, Ying He, Xinjuan Li, Zhengwei Liu, Keren Wang, Gaofeng Zhu, Wenmin Liu, Zhenghuai Tan & Zhipei Sang
Pages: 792-816
Published online: 22 Feb 2022
AbstractforDevelopment of naringenin-O-alkylamine derivatives as multifunctional agents for the treatment of Alzheimer’s disease | Full Text | References | PDF (5.9 MB) | EPUB | Supplemental
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Brief Reports

Brief Report
Discovery of novel paeonol-based derivatives against skin inflammation in vitro and in vivo
Jing Wu, Ren De Zhu, Guo Min Cao, Jun Cheng Du, Xin Liu, Liang Zhuo Diao, Zhao Yan Zhang, Yang Sheng Hu, Xin Hua Liu & Jing Bo Shi
Pages: 817-831
Published online: 28 Feb 2022
AbstractforDiscovery of novel paeonol-based derivatives against skin inflammation in vitro and in vivo | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 2554 Views
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Brief Report
Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors
Longjia Yan, Qin Wang, Li Liu & Yi Le
Pages: 832-843
Published online: 09 Mar 2022
AbstractforDesign, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Research Paper

Article
6-Amino-2,4,5-trimethylpyridin-3-ol and 2-amino-4,6-dimethylpyrimidin-5-ol derivatives as selective fibroblast growth factor receptor 4 inhibitors: design, synthesis, molecular docking, and anti-hepatocellular carcinoma efficacy evaluation
Chhabi Lal Chaudhary, Dongchul Lim, Prakash Chaudhary, Diwakar Guragain, Bhuwan Prasad Awasthi, Hee Dong Park, Jung-Ae Kim & Byeong-Seon Jeong
Pages: 844-856
Published online: 17 Mar 2022
Abstractfor6-Amino-2,4,5-trimethylpyridin-3-ol and 2-amino-4,6-dimethylpyrimidin-5-ol derivatives as selective fibroblast growth factor receptor 4 inhibitors: design, synthesis, molecular docking, and anti-hepatocellular carcinoma efficacy evaluation | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
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Brief Report

Brief Report
Diversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile
Tatiana Sharonova, Petr Zhmurov, Stanislav Kalinin, Alessio Nocentini, Andrea Angeli, Marta Ferraroni, Mikhail Korsakov, Claudiu T. Supuran & Mikhail Krasavin
Pages: 857-865
Published online: 16 Mar 2022
AbstractforDiversely substituted sulfamides for fragment-based drug discovery of carbonic anhydrase inhibitors: synthesis and inhibitory profile | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Research Paper

Article
Discovery of novel sulphonamide hybrids that inhibit LSD1 against bladder cancer cells
Jia Liu, Xingwang Zhu, Liu Yu & Minghuan Mao
Pages: 866-875
Published online: 30 Mar 2022
AbstractforDiscovery of novel sulphonamide hybrids that inhibit LSD1 against bladder cancer cells | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Review

Review
Echinocandins – structure, mechanism of action and use in antifungal therapy
Mateusz Szymański, Sandra Chmielewska, Urszula Czyżewska, Marta Malinowska & Adam Tylicki
Pages: 876-894
Published online: 16 Mar 2022
AbstractforEchinocandins – structure, mechanism of action and use in antifungal therapy | Full Text | References | PDF (4.8 MB) | EPUB
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Research Papers

Article
Pyrimidine-5-carbonitrile based potential anticancer agents as apoptosis inducers through PI3K/AKT axis inhibition in leukaemia K562
Nehad M. El-Dydamony, Rana M. Abdelnaby, Rasha Abdelhady, Omaima Ali, Mohamed I. Fahmy, Rasha R. Fakhr Eldeen & Amira A. Helwa
Pages: 895-911
Published online: 29 Mar 2022
AbstractforPyrimidine-5-carbonitrile based potential anticancer agents as apoptosis inducers through PI3K/AKT axis inhibition in leukaemia K562 | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
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Article
Drug-like molecules with anti-trypanothione synthetase activity identified by high throughput screening
Diego Benítez, Jaime Franco, Florencia Sardi, Alejandro Leyva, Rosario Durán, Gahee Choi, Gyongseon Yang, Taehee Kim, Namyoul Kim, Jinyeong Heo, Kideok Kim, Honggun Lee, Inhee Choi, Constantin Radu, David Shum, Joo Hwan No & Marcelo A. Comini
Pages: 912-929
Published online: 21 Mar 2022
AbstractforDrug-like molecules with anti-trypanothione synthetase activity identified by high throughput screening | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
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Brief Report

Brief Report
The three-tails approach as a new strategy to improve selectivity of action of sulphonamide inhibitors against tumour-associated carbonic anhydrase IX and XII
Alessandro Bonardi, Silvia Bua, Jacob Combs, Carrie Lomelino, Jacob Andring, Sameh Mohamed Osman, Alessandra Toti, Lorenzo Di Cesare Mannelli, Paola Gratteri, Carla Ghelardini, Robert McKenna, Alessio Nocentini & Claudiu T. Supuran
Pages: 930-939
Published online: 21 Mar 2022
AbstractforThe three-tails approach as a new strategy to improve selectivity of action of sulphonamide inhibitors against tumour-associated carbonic anhydrase IX and XII | Full Text | References | PDF (2.3 MB) | Supplemental
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Research Papers

Article
Rational design, optimization, and biological evaluation of novel α-Phosphonopropionic acids as covalent inhibitors of Rab geranylgeranyl transferase
Joanna Małolepsza, Aleksandra Marchwicka, Remigiusz A. Serwa, Sanna P. Niinivehmas, Olli T. Pentikäinen, Edyta Gendaszewska-Darmach & Katarzyna M. Błażewska
Pages: 940-951
Published online: 30 Mar 2022
AbstractforRational design, optimization, and biological evaluation of novel α-Phosphonopropionic acids as covalent inhibitors of Rab geranylgeranyl transferase | Full Text | References | PDF (4 MB) | EPUB | Supplemental
  • 1755 Views
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Article
Design and synthesis of benzodiazepines as brain penetrating PARP-1 inhibitors
Jiang Yu, Wenfeng Gou, Haihua Shang, Yating Cui, Xiao Sun, Lingling Luo, Wenbin Hou, Tiemin Sun & Yiliang Li
Pages: 952-972
Published online: 22 Mar 2022
AbstractforDesign and synthesis of benzodiazepines as brain penetrating PARP-1 inhibitors | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
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Article
Heterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity
Rossella Fioravanti, Veronica Rodriguez, Jonatan Caroli, Ugo Chianese, Rosaria Benedetti, Elisabetta Di Bello, Beatrice Noce, Clemens Zwergel, Davide Corinti, Dolores Viña, Lucia Altucci, Andrea Mattevi, Sergio Valente & Antonello Mai
Pages: 973-985
Published online: 22 Mar 2022
AbstractforHeterocycle-containing tranylcypromine derivatives endowed with high anti-LSD1 activity | Full Text | References | PDF (3.7 MB) | EPUB
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Brief Report

Brief Report
Biological investigation of N-methyl thiosemicarbazones as antimicrobial agents and bacterial carbonic anhydrases inhibitors
Ilaria D’Agostino, Githa Elizabeth Mathew, Paola Angelini, Roberto Venanzoni, Giancarlo Angeles Flores, Andrea Angeli, Simone Carradori, Beatrice Marinacci, Luigi Menghini, Mohamed A. Abdelgawad, Mohammed M. Ghoneim, Bijo Mathew & Claudiu T. Supuran
Pages: 986-993
Published online: 24 Mar 2022
AbstractforBiological investigation of N-methyl thiosemicarbazones as antimicrobial agents and bacterial carbonic anhydrases inhibitors | Full Text | References | PDF (2 MB) | EPUB
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Research Paper

Article
4-Anilinoquinazoline-based benzenesulfonamides as nanomolar inhibitors of carbonic anhydrase isoforms I, II, IX, and XII: design, synthesis, in-vitro, and in-silico biological studies
Hossam Nada, Ahmed Elkamhawy, Magda H. Abdellattif, Andrea Angeli, Chang Hoon Lee, Claudiu T. Supuran & Kyeong Lee
Pages: 994-1004
Published online: 30 Mar 2022
Abstractfor4-Anilinoquinazoline-based benzenesulfonamides as nanomolar inhibitors of carbonic anhydrase isoforms I, II, IX, and XII: design, synthesis, in-vitro, and in-silico biological studies | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
  • 1933 Views
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Brief Report

Brief Report
5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery
Stanislav Kalinin, Alexander Kovalenko, Annika Valtari, Alessio Nocentini, Maxim Gureev, Arto Urtti, Mikhail Korsakov, Claudiu T. Supuran & Mikhail Krasavin
Pages: 1005-1011
Published online: 30 Mar 2022
Abstractfor5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery | Full Text | References | PDF (2.1 MB) | Supplemental
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Article
Design, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease
Maja Przybyłowska, Krystyna Dzierzbicka, Szymon Kowalski, Sebastian Demkowicz, Mateusz Daśko & Iwona Inkielewicz-Stepniak
Pages: 1012-1022
Published online: 31 Mar 2022
AbstractforDesign, synthesis and biological evaluation of novel N-phosphorylated and O-phosphorylated tacrine derivatives as potential drugs against Alzheimer’s disease | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Review

Review
Natural source, bioactivity and synthesis of 3-Arylcoumarin derivatives
Qiang Zhang, Yu-hang Miao, Teng Liu, Yin-ling Yun, Xiao-ya Sun, Tao Yang & Jie Sun
Pages: 1023-1042
Published online: 19 Apr 2022
AbstractforNatural source, bioactivity and synthesis of 3-Arylcoumarin derivatives | Full Text | References | PDF (3.6 MB) | EPUB
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Research Papers

Article
Novel 3-(6-methylpyridin-2-yl)coumarin-based chalcones as selective inhibitors of cancer-related carbonic anhydrases IX and XII endowed with anti-proliferative activity
Haytham O. Tawfik, Moataz A. Shaldam, Alessio Nocentini, Rofaida Salem, Hadia Almahli, Sara T. Al-Rashood, Claudiu T. Supuran & Wagdy M. Eldehna
Pages: 1043-1052
Published online: 19 Apr 2022
AbstractforNovel 3-(6-methylpyridin-2-yl)coumarin-based chalcones as selective inhibitors of cancer-related carbonic anhydrases IX and XII endowed with anti-proliferative activity | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1905 Views
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Article
Design, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers
Heba S. A. Elzahabi, Eman S. Nossier, Rania A. Alasfoury, May El-Manawaty, Sara M. Sayed, Eslam B. Elkaeed, Ahmed M. Metwaly, Mohamed Hagras & Ibrahim H. Eissa
Pages: 1053-1076
Published online: 12 Jul 2022
AbstractforDesign, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers | Full Text | References | PDF (6.7 MB) | EPUB | Supplemental
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Brief Report

Brief Report
Bat coronaviruses related to SARS-CoV-2: what about their 3CL proteases (MPro)?
Matteo Pavan, Davide Bassani, Mattia Sturlese & Stefano Moro
Pages: 1077-1082
Published online: 13 Apr 2022
AbstractforBat coronaviruses related to SARS-CoV-2: what about their 3CL proteases (MPro)? | Full Text | References | PDF (1.5 MB) | EPUB
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Research Papers

Article
Interactions of 2,6-substituted purines with purine nucleoside phosphorylase from Helicobacter pylori in solution and in the crystal, and the effects of these compounds on cell cultures of this bacterium
Marta Narczyk, Marta Ilona Wojtyś, Ivana Leščić Ašler, Biserka Žinić, Marija Luić, Elżbieta Katarzyna Jagusztyn-Krynicka, Zoran Štefanić & Agnieszka Bzowska
Pages: 1083-1097
Published online: 18 Apr 2022
AbstractforInteractions of 2,6-substituted purines with purine nucleoside phosphorylase from Helicobacter pylori in solution and in the crystal, and the effects of these compounds on cell cultures of this bacterium | Full Text | References | PDF (4.8 MB) | EPUB | Supplemental
  • 1371 Views
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Article
Ligand-based design and synthesis of N'-Benzylidene-3,4-dimethoxybenzohydrazide derivatives as potential antimicrobial agents; evaluation by in vitro, in vivo, and in silico approaches with SAR studies
Rogy R. Ezz Eldin, Marwa A. Saleh, Mohammad Hayal Alotaibi, Reem K. Alsuair, Yahya A. Alzahrani, Feras A. Alshehri, Amany F. Mohamed, Shaimaa M. Hafez, Azza Ali Althoqapy, Seham K. Khirala, Mona M. Amin, Yousuf A. F, Azza H. AbdElwahab, Mohamed S. Alesawy, Ayman Abo Elmaaty & Ahmed A. Al-Karmalawy
Pages: 1098-1119
Published online: 18 Apr 2022
AbstractforLigand-based design and synthesis of N'-Benzylidene-3,4-dimethoxybenzohydrazide derivatives as potential antimicrobial agents; evaluation by in vitro, in vivo, and in silico approaches with SAR studies | Full Text | References | PDF (7.1 MB) | EPUB | Supplemental
  • 2755 Views
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Review

Review
Paving the way towards effective plant-based inhibitors of hyaluronidase and tyrosinase: a critical review on a structure–activity relationship
Jakub Gębalski, Filip Graczyk & Daniel Załuski
Pages: 1120-1195
Published online: 26 Apr 2022
AbstractforPaving the way towards effective plant-based inhibitors of hyaluronidase and tyrosinase: a critical review on a structure–activity relationship | Full Text | References | PDF (8.5 MB) | EPUB
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Research Papers

Article
Design, synthesis, and molecular docking studies of novel pomalidomide-based PROTACs as potential anti-cancer agents targeting EGFRWT and EGFRT790M
Moustafa O. Aboelez, Amany Belal, Guangya Xiang & Xiang Ma
Pages: 1196-1211
Published online: 26 Apr 2022
AbstractforDesign, synthesis, and molecular docking studies of novel pomalidomide-based PROTACs as potential anti-cancer agents targeting EGFRWT and EGFRT790M | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
  • 4159 Views
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Article
Design, synthesis, and cytotoxic activities of isaindigotone derivatives as potential anti-gastric cancer agents
Kangjia Du, Wantong Ma, Chengjie Yang, Zhongkun Zhou, Shujian Hu, Yanan Tian, Hao Zhang, Yunhao Ma, Xinrong Jiang, Hongmei Zhu, Huanxiang Liu, Peng Chen & Yingqian Liu
Pages: 1212-1226
Published online: 21 Apr 2022
AbstractforDesign, synthesis, and cytotoxic activities of isaindigotone derivatives as potential anti-gastric cancer agents | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 2335 Views
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Article
Identification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights
Wagdy M. Eldehna, Raed M. Maklad, Hadia Almahli, Tarfah Al-Warhi, Eslam B. Elkaeed, Mohammed A. S. Abourehab, Hatem A. Abdel-Aziz & Ahmed M. El Kerdawy
Pages: 1227-1240
Published online: 26 Apr 2022
AbstractforIdentification of 3-(piperazinylmethyl)benzofuran derivatives as novel type II CDK2 inhibitors: design, synthesis, biological evaluation, and in silico insights | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 3051 Views
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Article
Novel Sunifiram-carbamate hybrids as potential dual acetylcholinesterase inhibitor and NMDAR co-agonist: simulation-guided analogue design and pharmacological screening
Khalid A. Agha, Nader E. Abo-Dya, Abdul Rashid Issahaku, Clement Agoni, Mahmoud E. S. Soliman, Eatedal H. Abdel-Aal, Zakaria K. Abdel-Samii & Tarek S. Ibrahim
Pages: 1241-1256
Published online: 28 Apr 2022
AbstractforNovel Sunifiram-carbamate hybrids as potential dual acetylcholinesterase inhibitor and NMDAR co-agonist: simulation-guided analogue design and pharmacological screening | Full Text | References | PDF (4.3 MB) | EPUB | Supplemental
  • 1678 Views
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Article
Identification of highly selective type II kinase inhibitors with chiral peptidomimetic tails
Seo-Jung Han, Jae Eun Jung, Do Hee Oh, Minsup Kim, Jae-Min Kim, Kyung-Sook Chung, Hee-Soo Han, Jeong-Hun Lee, Kyung-Tae Lee, Hee Jin Jeong, In Ho Park, Eunkyeong Jeon, Jeon-Soo Shin, Dongkeun Hwang, Art E. Cho, Duck-Hyung Lee & Taebo Sim
Pages: 1257-1277
Published online: 28 Apr 2022
AbstractforIdentification of highly selective type II kinase inhibitors with chiral peptidomimetic tails | Full Text | References | PDF (3.2 MB) | Supplemental
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Review

Review
Targeting carbonic anhydrase IX and XII isoforms with small molecule inhibitors and monoclonal antibodies
Mateusz Kciuk, Adrianna Gielecińska, Somdutt Mujwar, Mariusz Mojzych, Beata Marciniak, Rafał Drozda & Renata Kontek
Pages: 1278-1298
Published online: 04 May 2022
AbstractforTargeting carbonic anhydrase IX and XII isoforms with small molecule inhibitors and monoclonal antibodies | Full Text | References | PDF (3.3 MB) | EPUB
  • 4580 Views
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Brief Reports

Brief Report
Design, synthesis and biological evaluation of novel diosgenin–benzoic acid mustard hybrids with potential anti-proliferative activities in human hepatoma HepG2 cells
Jinling Zhang, Wenbao Wang, Yanzhao Tian, Liwei Ma, Lin Zhou, Hao Sun, Yukun Ma, Huiling Hou, Xiaoli Wang, Jin Ye & Xiaobo Wang
Pages: 1299-1314
Published online: 02 Jun 2022
AbstractforDesign, synthesis and biological evaluation of novel diosgenin–benzoic acid mustard hybrids with potential anti-proliferative activities in human hepatoma HepG2 cells | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 1973 Views
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Brief Report
Phosphorus containing analogues of SAHA as inhibitors of HDACs
Michael D. Pun, Hsin-Hua Wu, Feyisola P. Olatunji, Britany N. Kesic, John W. Peters & Clifford E. Berkman
Pages: 1315-1319
Published online: 05 May 2022
AbstractforPhosphorus containing analogues of SAHA as inhibitors of HDACs | Full Text | References | PDF (1 MB) | EPUB | Supplemental
  • 1616 Views
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Brief Report
Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase
Supreet Kaur, Nicholas S. Nieto, Peter McDonald, Josh R. Beck, Richard B. Honzatko, Anuradha Roy & Scott W. Nelson
Pages: 1320-1326
Published online: 05 May 2022
AbstractforDiscovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 1735 Views
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Research Papers

Article
Design, synthesis, biological evaluation and QSAR analysis of novel N-substituted benzimidazole derived carboxamides
Anja Beč, Marija Mioč, Branimir Bertoša, Marija Kos, Patricia Debogović, Marijeta Kralj, Kristina Starčević & Marijana Hranjec
Pages: 1327-1339
Published online: 06 May 2022
AbstractforDesign, synthesis, biological evaluation and QSAR analysis of novel N-substituted benzimidazole derived carboxamides | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1880 Views
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Article
The inhibitory effect of boric acid on hypoxia-regulated tumour-associated carbonic anhydrase IX
Zainab Saad Yusuf, Tugba Kevser Uysal, Ender Simsek, Alessio Nocentini, Sameh Mohamed Osman, Claudiu T. Supuran & Özen Özensoy Güler
Pages: 1340-1345
Published online: 10 May 2022
AbstractforThe inhibitory effect of boric acid on hypoxia-regulated tumour-associated carbonic anhydrase IX | Full Text | References | PDF (1 MB) | EPUB
  • 1921 Views
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Article
New 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I& II and tubulin polymerization
Hamada H. H. Mohammed, Amer Ali Abd El-Hafeez, Kareem Ebeid, Aml I. Mekkawy, Mohammed A. S. Abourehab, Emad I. Wafa, Suhaila O. Alhaj-Suliman, Aliasger K. Salem, Pradipta Ghosh, Gamal El-Din A. Abuo-Rahma, Alaa M. Hayallah & Samar H. Abbas
Pages: 1346-1363
Published online: 11 May 2022
AbstractforNew 1,2,3-triazole linked ciprofloxacin-chalcones induce DNA damage by inhibiting human topoisomerase I& II and tubulin polymerization | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 2896 Views
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Article
sp2-Iminosugars targeting human lysosomal β-hexosaminidase as pharmacological chaperone candidates for late-onset Tay-Sachs disease
Manuel González-Cuesta, Irene Herrera-González, M. Isabel García-Moreno, Roger A. Ashmus, David J. Vocadlo, José M. García Fernández, Eiji Nanba, Katsumi Higaki & Carmen Ortiz Mellet
Pages: 1364-1374
Published online: 16 May 2022
Abstractforsp2-Iminosugars targeting human lysosomal β-hexosaminidase as pharmacological chaperone candidates for late-onset Tay-Sachs disease | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
  • 2038 Views
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Article
Design, synthesis, and evaluation of novel O-alkyl ferulamide derivatives as multifunctional ligands for treating Alzheimer’s disease
Gaofeng Zhu, Ping Bai, Keren Wang, Jing Mi, Jing Yang, Jiaqi Hu, Yujuan Ban, Ran Xu, Rui Chen, Changning Wang, Lei Tang & Zhipei Sang
Pages: 1375-1388
Published online: 13 May 2022
AbstractforDesign, synthesis, and evaluation of novel O-alkyl ferulamide derivatives as multifunctional ligands for treating Alzheimer’s disease | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
  • 2035 Views
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Article
Discovery of new nicotinamides as apoptotic VEGFR-2 inhibitors: virtual screening, synthesis, anti-proliferative, immunomodulatory, ADMET, toxicity, and molecular dynamic simulation studies
Reda G. Yousef, Albaraa Ibrahim, Mohamed M. Khalifa, Wagdy M. Eldehna, Ibraheem M. M. Gobaara, Ahmed B. M. Mehany, Eslam B. Elkaeed, Aisha A. Alsfouk, Ahmed M. Metwaly & Ibrahim H. Eissa
Pages: 1389-1403
Published online: 16 May 2022
AbstractforDiscovery of new nicotinamides as apoptotic VEGFR-2 inhibitors: virtual screening, synthesis, anti-proliferative, immunomodulatory, ADMET, toxicity, and molecular dynamic simulation studies | Full Text | References | PDF (4.7 MB) | EPUB | Supplemental
  • 2186 Views
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Brief Report

Brief Report
From Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica
Alessio Ottaviani, Joshua Welsch, Keli Agama, Yves Pommier, Alessandro Desideri, Bill J. Baker & Paola Fiorani
Pages: 1404-1410
Published online: 23 May 2022
AbstractforFrom Antarctica to cancer research: a novel human DNA topoisomerase 1B inhibitor from Antarctic sponge Dendrilla antarctica | Full Text | References | PDF (1.4 MB) | EPUB
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Research Papers

Article
Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as novel and potent TBK1 inhibitors: design, synthesis, biological evaluation, and molecular docking study
Yin Sun, Haotian Tang, Xiaoyan Wang, Fang Feng, Tiantian Fan, Dongmei Zhao, Bing Xiong, Hua Xie & Tongchao Liu
Pages: 1411-1425
Published online: 19 May 2022
AbstractforIdentification of 1H-pyrazolo[3,4-b]pyridine derivatives as novel and potent TBK1 inhibitors: design, synthesis, biological evaluation, and molecular docking study | Full Text | References | PDF (5.9 MB) | EPUB | Supplemental
  • 2456 Views
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Article
Models of enzyme inhibition and apparent dissociation constants from kinetic analysis to study the differential inhibition of aldose reductase
Francesco Balestri, Mario Cappiello, Roberta Moschini, Umberto Mura & Antonella Del-Corso
Pages: 1426-1436
Published online: 24 May 2022
AbstractforModels of enzyme inhibition and apparent dissociation constants from kinetic analysis to study the differential inhibition of aldose reductase | Full Text | References | PDF (1.9 MB) | EPUB
  • 1231 Views
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Review

Review
Recent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents
Chao Wang, Yujing Zhang, Lingyu Shi, Shanbo Yang, Jing Chang, Yingjie Zhong, Qian Li & Dongming Xing
Pages: 1437-1453
Published online: 19 May 2022
AbstractforRecent advances in IAP-based PROTACs (SNIPERs) as potential therapeutic agents | Full Text | References | PDF (2.9 MB) | EPUB
  • 4361 Views
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Research Papers

Article
Selective inhibition of carbonic anhydrase IX by sulphonylated 1,2,3-triazole incorporated benzenesulphonamides capable of inducing apoptosis
Kiran Siwach, Amit Kumar, Harish Panchal, Rajiv Kumar, Jitender Kumar Bhardwaj, Andrea Angeli, Claudiu T. Supuran & Pawan K. Sharma
Pages: 1454-1463
Published online: 26 May 2022
AbstractforSelective inhibition of carbonic anhydrase IX by sulphonylated 1,2,3-triazole incorporated benzenesulphonamides capable of inducing apoptosis | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 1242 Views
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Article
Synthesis, X-ray diffraction analysis, quantum chemical studies and α-amylase inhibition of probenecid derived S-alkylphthalimide-oxadiazole-benzenesulfonamide hybrids
Bilal Ahmad Khan, Syeda Shamila Hamdani, Muhammad Naeem Ahmed, Shahid Hameed, Muhammad Ashfaq, Ahmed M. Shawky, Mahmoud A. A. Ibrahim & Peter A. Sidhom
Pages: 1464-1478
Published online: 26 May 2022
AbstractforSynthesis, X-ray diffraction analysis, quantum chemical studies and α-amylase inhibition of probenecid derived S-alkylphthalimide-oxadiazole-benzenesulfonamide hybrids | Full Text | References | PDF (3.5 MB) | EPUB
  • 1679 Views
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Article
Development of Praziquantel sulphonamide derivatives as antischistosomal drugs
Andrea Angeli, Marta Ferraroni, Fabrizio Carta, Cécile Häberli, Jennifer Keiser, Gabriele Costantino & Claudiu T. Supuran
Pages: 1479-1494
Published online: 29 May 2022
AbstractforDevelopment of Praziquantel sulphonamide derivatives as antischistosomal drugs | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 1183 Views
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Article
Design, synthesis and biological evaluation of novel triazoloquinazolinone and imidazoquinazolinone derivatives as allosteric inhibitors of SHP2 phosphatase
Wenjun Ye, Ye Liu, Qian Ren, Tianhui Liao, Yumei Chen, Dongmei Chen, Sisi Wang, Lihong Yao, Yihe Jia, Chunshen Zhao & Zhixu Zhou
Pages: 1495-1513
Published online: 29 May 2022
AbstractforDesign, synthesis and biological evaluation of novel triazoloquinazolinone and imidazoquinazolinone derivatives as allosteric inhibitors of SHP2 phosphatase | PDF (3.5 MB) | Supplemental
  • 477 Views
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Article
Design, synthesis, and biological evaluation of triazole-pyrimidine-methylbenzonitrile derivatives as dual A2A/A2B adenosine receptor antagonists
Zhi Li, Lijuan Kou, Xinzhen Fu, Zeping Xie, Maolei Xu, Lin Guo, Tiantian Lin, Shizhou Gong, Shumin Zhang & Ming Liu
Pages: 1514-1526
Published online: 26 May 2022
AbstractforDesign, synthesis, and biological evaluation of triazole-pyrimidine-methylbenzonitrile derivatives as dual A2A/A2B adenosine receptor antagonists | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 1834 Views
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Article
Automated approach for the evaluation of glutathione-S-transferase P1-1 inhibition by organometallic anticancer compounds
Sarah A. P. Pereira, A. Catarina Baptista L, Lorenzo Biancalana, Fabio Marchetti, Paul J. Dyson & M. Lúcia M. F. S. Saraiva
Pages: 1527-1536
Published online: 29 May 2022
AbstractforAutomated approach for the evaluation of glutathione-S-transferase P1-1 inhibition by organometallic anticancer compounds | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
  • 1246 Views
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Article
Design, synthesis, and biological evaluation of novel carbazole derivatives as potent DNMT1 inhibitors with reasonable PK properties
Ennian Li, Kai Wang, Bei Zhang, Siqi Guo, Senhao Xiao, Qi Pan, Xiaowan Wang, Weiying Chen, Yunshan Wu, Hesong Xu, Xiangqian Kong, Cheng Luo, Shijie Chen & Bo Liu
Pages: 1537-1555
Published online: 07 Jun 2022
AbstractforDesign, synthesis, and biological evaluation of novel carbazole derivatives as potent DNMT1 inhibitors with reasonable PK properties | Full Text | References | PDF (3.8 MB) | EPUB | Supplemental
  • 2348 Views
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Article
Triazoloquinoxalines-based DNA intercalators-Topo II inhibitors: design, synthesis, docking, ADMET and anti-proliferative evaluations
Alaa Elwan, Helmy Sakr, Abdel-Ghany A. El-Helby, Ahmed El-morsy, Mohamed A. Abdelgawad, Mohammed M. Ghoneim, Mohamed El-Sherbiny & Khaled El-Adl
Pages: 1556-1567
Published online: 29 May 2022
AbstractforTriazoloquinoxalines-based DNA intercalators-Topo II inhibitors: design, synthesis, docking, ADMET and anti-proliferative evaluations | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
  • 1178 Views
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Article
4-(3-Alkyl/benzyl-guanidino)benzenesulfonamides as selective carbonic anhydrase VII inhibitors
Morteza Abdoli, Simone Giovannuzzi, Claudiu T. Supuran & Raivis Žalubovskis
Pages: 1568-1576
Published online: 29 May 2022
Abstractfor4-(3-Alkyl/benzyl-guanidino)benzenesulfonamides as selective carbonic anhydrase VII inhibitors | Full Text | References | PDF (3 MB)
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Original Article

Article
Cloning, purification, kinetic and anion inhibition studies of a recombinant β-carbonic anhydrase from the Atlantic salmon parasite platyhelminth Gyrodactylus salaris
Ashok Aspatwar, Harlan Barker, Heidi Aisala, Ksenia Zueva, Marianne Kuuslahti, Martti Tolvanen, Craig R. Primmer, Jaakko Lumme, Alessandro Bonardi, Amit Tripathi, Seppo Parkkila & Claudiu T. Supuran
Pages: 1577-1586
Published online: 30 May 2022
AbstractforCloning, purification, kinetic and anion inhibition studies of a recombinant β-carbonic anhydrase from the Atlantic salmon parasite platyhelminth Gyrodactylus salaris | Full Text | References | PDF (3 MB) | EPUB
  • 1320 Views
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Article
Design, synthesis, molecular modeling and biological evaluation of novel Benzoxazole-Benzamide conjugates via a 2-Thioacetamido linker as potential anti-proliferative agents, VEGFR-2 inhibitors and apoptotic inducers
Ibrahim H. Eissa, Radwan El-Haggar, Mohammed A. Dahab, Marwa F. Ahmed, Hazem A. Mahdy, Reem I. Alsantali, Alaa Elwan, Nicolas Masurier & Samar S. Fatahala
Pages: 1587-1599
Published online: 30 May 2022
AbstractforDesign, synthesis, molecular modeling and biological evaluation of novel Benzoxazole-Benzamide conjugates via a 2-Thioacetamido linker as potential anti-proliferative agents, VEGFR-2 inhibitors and apoptotic inducers | Full Text | References | PDF (3 MB) | EPUB | Supplemental
  • 1747 Views
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Article
Interaction of letrozole and its degradation products with aromatase: chemometric assessment of kinetics and structure-based binding validation
Michele De Luca, Maria Antonietta Occhiuzzi, Bruno Rizzuti, Giuseppina Ioele, Gaetano Ragno, Antonio Garofalo & Fedora Grande
Pages: 1600-1609
Published online: 29 May 2022
AbstractforInteraction of letrozole and its degradation products with aromatase: chemometric assessment of kinetics and structure-based binding validation | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 1361 Views
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Article
GC/MS analysis and potential synergistic effect of mandarin and marjoram oils on Helicobacter pylori
Rawah H. Elkousy, Nada M. Mostafa, Ahmed M. Abd-alkhalek, Mahmoud A. El Hassab, Sara T. Al-Rashood, Wagdy M. Eldehna & Omayma A. Eldahshan
Pages: 1610-1619
Published online: 31 May 2022
AbstractforGC/MS analysis and potential synergistic effect of mandarin and marjoram oils on Helicobacter pylori | Full Text | References | PDF (2.2 MB) | EPUB
  • 1973 Views
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Article
Discovery of N-quinazolinone-4-hydroxy-2-quinolone-3-carboxamides as DNA gyrase B-targeted antibacterial agents
Wenjie Xue, Yaling Wang, Xu Lian, Xueyao Li, Jing Pang, Johannes Kirchmair, Kebin Wu, Zunsheng Han, Xuefu You, Hongmin Zhang, Jie Xia & Song Wu
Pages: 1620-1631
Published online: 07 Jun 2022
AbstractforDiscovery of N-quinazolinone-4-hydroxy-2-quinolone-3-carboxamides as DNA gyrase B-targeted antibacterial agents | Full Text | References | PDF (2 MB) | EPUB | Supplemental
  • 1653 Views
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Article
Design and biological evaluation of substituted 5,7-dihydro-6H-indolo[2,3-c]quinolin-6-one as novel selective Haspin inhibitors
Sreenivas Avula, Xudan Peng, Xingfen Lang, Micky Tortorella, Béatrice Josselin, Stéphane Bach, Stephane Bourg, Pascal Bonnet, Frédéric Buron, Sandrine Ruchaud, Sylvain Routier & Cleopatra Neagoie
Pages: 1632-1650
Published online: 07 Jun 2022
AbstractforDesign and biological evaluation of substituted 5,7-dihydro-6H-indolo[2,3-c]quinolin-6-one as novel selective Haspin inhibitors | Full Text | References | PDF (4.6 MB) | EPUB | Supplemental
  • 2184 Views
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Article
A comparative study of carbonic anhydrase activity in lymphocytes from colorectal cancer tissues and adjacent healthy counterparts
Giulia Nannini, Viviana De Luca, Chiara D’Ambrosio, Andrea Scaloni, Antonio Taddei, Maria Novella Ringressi, Fabio Cianchi, Fabio Staderini, Clemente Capasso, Amedeo Amedei & Claudiu T. Supuran
Pages: 1651-1655
Published online: 13 Jun 2022
AbstractforA comparative study of carbonic anhydrase activity in lymphocytes from colorectal cancer tissues and adjacent healthy counterparts | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
  • 1703 Views
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Article
Development of PD3 and PD3-B for PDEδ inhibition to modulate KRAS activity
Jungeun Lee, Ho Jin Lee, Yeongcheol Lee, Bumhee Lim, Jongsik Gam, Dong-Chan Oh & Jeeyeon Lee
Pages: 1656-1666
Published online: 13 Jun 2022
AbstractforDevelopment of PD3 and PD3-B for PDEδ inhibition to modulate KRAS activity | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Reviews

Review
Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges
Chao Wang, Yujing Zhang, Tingting Zhang, Lingyu Shi, Zhongmin Geng & Dongming Xing
Pages: 1667-1693
Published online: 14 Jun 2022
AbstractforProteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges | Full Text | References | PDF (5.3 MB) | EPUB
  • 3838 Views
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Review
PROTACs for BRDs proteins in cancer therapy: a review
Chao Wang, Yujing Zhang, Shanbo Yang, Wujun Chen & Dongming Xing
Pages: 1694-1703
Published online: 14 Jun 2022
AbstractforPROTACs for BRDs proteins in cancer therapy: a review | Full Text | References | PDF (1.9 MB) | EPUB
  • 2962 Views
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Research Papers

Article
From the Wuhan-Hu-1 strain to the XD and XE variants: is targeting the SARS-CoV-2 spike protein still a pharmaceutically relevant option against COVID-19?
Matteo Pavan, Davide Bassani, Mattia Sturlese & Stefano Moro
Pages: 1704-1714
Published online: 13 Jun 2022
AbstractforFrom the Wuhan-Hu-1 strain to the XD and XE variants: is targeting the SARS-CoV-2 spike protein still a pharmaceutically relevant option against COVID-19? | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 2805 Views
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Article
Design, synthesis, and biological evaluation of a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon modulators
Yilin Liu, Yuming Song, Yingju Xu, Meixu Jiang & Haibin Lu
Pages: 1715-1723
Published online: 14 Jun 2022
AbstractforDesign, synthesis, and biological evaluation of a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon modulators | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
  • 1936 Views
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Article
Synthesis and biological evaluation of thieno[3,2-c]pyrazol-3-amine derivatives as potent glycogen synthase kinase 3β inhibitors for Alzheimer’s disease
Ning Yan, Xiao-Long Shi, Long-Qian Tang, De-Feng Wang, Xun Li, Chao Liu & Zhao-Peng Liu
Pages: 1724-1736
Published online: 14 Jun 2022
AbstractforSynthesis and biological evaluation of thieno[3,2-c]pyrazol-3-amine derivatives as potent glycogen synthase kinase 3β inhibitors for Alzheimer’s disease | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
  • 2442 Views
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Article
Rational design of biodegradable sulphonamide candidates treating septicaemia by synergistic dual inhibition of COX-2/PGE2 axis and DHPS enzyme
Nada H. El-Dershaby, Soad A. El-Hawash, Shaymaa E. Kassab, Hoda G. Dabees, Ahmed E. Abdel Moneim, Ibrahim A. Abdel Wahab, Mohammad M. Abd-Alhaseeb & Mostafa M. M. El-Miligy
Pages: 1737-1751
Published online: 16 Jun 2022
AbstractforRational design of biodegradable sulphonamide candidates treating septicaemia by synergistic dual inhibition of COX-2/PGE2 axis and DHPS enzyme | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1733 Views
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Article
Synthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit
Lisa Vieider, Eva Zoeller, Erik Romp, Martin Schoenthaler, Victor Hernández-Olmos, Veronika Temml, Thomas Hasenoehrl, Daniela Schuster, Oliver Werz, Ulrike Garscha & Barbara Matuszczak
Pages: 1752-1764
Published online: 20 Sep 2022
AbstractforSynthesis and structure–activity relationships for some novel diflapolin derivatives with benzimidazole subunit | Full Text | References | PDF (2.6 MB) | EPUB
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Brief Report

Brief Report
Predicting potentially pathogenic effects of hRPE65 missense mutations: a computational strategy based on molecular dynamics simulations
Giulio Poli, Ivana Barravecchia, Gian Carlo Demontis, Andrea Sodi, Alessandro Saba, Stanislao Rizzo, Marco Macchia & Tiziano Tuccinardi
Pages: 1765-1772
Published online: 21 Jun 2022
AbstractforPredicting potentially pathogenic effects of hRPE65 missense mutations: a computational strategy based on molecular dynamics simulations | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
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Article
Structure-based optimization of type III indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors
Ute F. Röhrig, Somi Reddy Majjigapu, Pierre Vogel, Aline Reynaud, Florence Pojer, Nahzli Dilek, Patrick Reichenbach, Kelly Ascenção, Melita Irving, George Coukos, Olivier Michielin & Vincent Zoete
Pages: 1773-1811
Published online: 27 Jun 2022
AbstractforStructure-based optimization of type III indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors | Full Text | References | PDF (7.1 MB) | EPUB | Supplemental
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Brief Report

Brief Report
Pterostilbene fluorescent probes as potential tools for targeting neurodegeneration in biological applications
Lidia Ciccone, Susanna Nencetti, Maria Marino, Chiara Battocchio, Giovanna Iucci, Iole Venditti, Martina Marsotto, Emiliano Montalesi, Simone Socci, Beatrice Bargagna & Elisabetta Orlandini
Pages: 1812-1820
Published online: 27 Jun 2022
AbstractforPterostilbene fluorescent probes as potential tools for targeting neurodegeneration in biological applications | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Research Papers

Article
Novel pyrrolopyrimidine derivatives: design, synthesis, molecular docking, molecular simulations and biological evaluations as antioxidant and anti-inflammatory agents
Amira I. Sayed, Yara E. Mansour, Mohamed A. Ali, Omnia Aly, Zainab M. Khoder, Ahmed M. Said, Samar S. Fatahala & Rania H. Abd El-Hameed
Pages: 1821-1837
Published online: 27 Jun 2022
AbstractforNovel pyrrolopyrimidine derivatives: design, synthesis, molecular docking, molecular simulations and biological evaluations as antioxidant and anti-inflammatory agents | Full Text | References | PDF (2.8 MB) | EPUB
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Article
Structure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases
Weiwei An, Katrina J. Holly, Alessio Nocentini, Ryan D. Imhoff, Chad. S. Hewitt, Nader S. Abutaleb, Xufeng Cao, Mohamed N. Seleem, Claudiu T. Supuran & Daniel P. Flaherty
Pages: 1838-1844
Published online: 27 Jun 2022
AbstractforStructure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases | Full Text | References | PDF (3.2 MB) | EPUB
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Article
Dyhidro-β-agarofurans natural and synthetic as acetylcholinesterase and COX inhibitors: interaction with the peripheral anionic site (AChE-PAS), and anti-inflammatory potentials
Julio Alarcón-Enos, Evelyn Muñoz-Núñez, Margarita Gutiérrez, Soledad Quiroz-Carreño, Edgar Pastene-Navarrete & Carlos Céspedes Acuña
Pages: 1845-1856
Published online: 10 Jul 2022
AbstractforDyhidro-β-agarofurans natural and synthetic as acetylcholinesterase and COX inhibitors: interaction with the peripheral anionic site (AChE-PAS), and anti-inflammatory potentials | Full Text | References | PDF (1.7 MB) | EPUB
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Brief Reports

Brief Report
Benzenesulfonamides with different rigidity-conferring linkers as carbonic anhydrase inhibitors: an insight into the antiproliferative effect on glioblastoma, pancreatic, and breast cancer cells
Francesco Liguori, Simone Carradori, Roberto Ronca, Sara Rezzola, Serena Filiberti, Fabrizio Carta, Marta Turati & Claudiu T. Supuran
Pages: 1857-1869
Published online: 29 Jun 2022
AbstractforBenzenesulfonamides with different rigidity-conferring linkers as carbonic anhydrase inhibitors: an insight into the antiproliferative effect on glioblastoma, pancreatic, and breast cancer cells | Full Text | References | PDF (1.9 MB) | Supplemental
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Brief Report
Anti-breast cancer sinomenine derivatives via mechanisms of apoptosis induction and metastasis reduction
Xiang Gao, Baojia Sun, Yonglian Hou, Lilin Liu, Jianan Sun, Fanxing Xu, Dahong Li & Huiming Hua
Pages: 1870-1883
Published online: 08 Jul 2022
AbstractforAnti-breast cancer sinomenine derivatives via mechanisms of apoptosis induction and metastasis reduction | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
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Research Papers

Article
Design, synthesis and molecular docking of new fused 1H-pyrroles, pyrrolo[3,2-d]pyrimidines and pyrrolo[3,2-e][1, 4]diazepine derivatives as potent EGFR/CDK2 inhibitors
Amany Belal, Nagwa M. Abdel Gawad, Ahmed B. M. Mehany, Mohammed A. S. Abourehab, Hazem Elkady, Ahmed A. Al‐Karmalawy & Ahmed S. Ismael
Pages: 1884-1902
Published online: 08 Jul 2022
AbstractforDesign, synthesis and molecular docking of new fused 1H-pyrroles, pyrrolo[3,2-d]pyrimidines and pyrrolo[3,2-e][1, 4]diazepine derivatives as potent EGFR/CDK2 inhibitors | Full Text | References | PDF (4.8 MB) | EPUB | Supplemental
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Article
Design and synthesis of thiazolidine-2,4-diones hybrids with 1,2-dihydroquinolones and 2-oxindoles as potential VEGFR-2 inhibitors: in-vitro anticancer evaluation and in-silico studies
Mohammed S. Taghour, Hazem Elkady, Wagdy M. Eldehna, Nehal M. El-Deeb, Ahmed M. Kenawy, Eslam B. Elkaeed, Aisha A. Alsfouk, Mohamed S. Alesawy, Ahmed M. Metwaly & Ibrahim. H. Eissa
Pages: 1903-1917
Published online: 08 Jul 2022
AbstractforDesign and synthesis of thiazolidine-2,4-diones hybrids with 1,2-dihydroquinolones and 2-oxindoles as potential VEGFR-2 inhibitors: in-vitro anticancer evaluation and in-silico studies | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
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Article
Discovery and SAR analysis of 5-chloro-4-((substituted phenyl)amino)pyrimidine bearing histone deacetylase inhibitors
Lin Zhang, Yiming Chen, Fahui Li, Lihui Zhang, Jinhong Feng & Lei Zhang
Pages: 1918-1927
Published online: 14 Jul 2022
AbstractforDiscovery and SAR analysis of 5-chloro-4-((substituted phenyl)amino)pyrimidine bearing histone deacetylase inhibitors | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
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Review

Review
Inhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties
Joanna Stefaniak, Michał G. Nowak, Marek Wojciechowski, Sławomir Milewski & Andrzej S. Skwarecki
Pages: 1928-1956
Published online: 08 Jul 2022
AbstractforInhibitors of glucosamine-6-phosphate synthase as potential antimicrobials or antidiabetics – synthesis and properties | Full Text | References | PDF (4.8 MB) | EPUB
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Research Papers

Article
Synthesis, biological evaluation, and in silico studies of new CDK2 inhibitors based on pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold with apoptotic activity
Asmaa A. Mandour, Ibrahim F. Nassar, Mohammed T. Abdel Aal, Mahmoud A. E. Shahin, Wael A. El-Sayed, Maghawry Hegazy, Amr Mohamed Yehia, Ahmed Ismail, Mohamed Hagras, Eslam B. Elkaeed, Hanan M. Refaat & Nasser S. M. Ismail
Pages: 1957-1973
Published online: 10 Jul 2022
AbstractforSynthesis, biological evaluation, and in silico studies of new CDK2 inhibitors based on pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold with apoptotic activity | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
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Article
GC-MS metabolites profiling of anethole-rich oils by different extraction techniques: antioxidant, cytotoxicity and in-silico enzymes inhibitory insights
Dina M. El-Kersh, Nada M. Mostafa, Shaimaa Fayez, Tarfah Al-Warhi, Mohammed A. S. Abourehab, Wagdy M. Eldehna & Mohamed A. Salem
Pages: 1974-1986
Published online: 18 Jul 2022
AbstractforGC-MS metabolites profiling of anethole-rich oils by different extraction techniques: antioxidant, cytotoxicity and in-silico enzymes inhibitory insights | Full Text | References | PDF (2.8 MB) | EPUB
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Brief Report

Brief Report
Discovery of a new class of triazole based inhibitors of acetyl transferase KAT2A
Roberta Pacifico, Nunzio Del Gaudio, Guglielmo Bove, Lucia Altucci, Lydia Siragusa, Gabriele Cruciani, Menotti Ruvo, Rosa Bellavita, Paolo Grieco & Mauro F. A. Adamo
Pages: 1987-1994
Published online: 25 Jul 2022
AbstractforDiscovery of a new class of triazole based inhibitors of acetyl transferase KAT2A | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Research Papers

Article
Discovery of novel mRNA demethylase FTO inhibitors against esophageal cancer
Bo Qin, Qian Bai, Dan Yan, Fanxiang Yin, Zhu Zhu, Chaoyuan Xia, Yang Yang & Yi Zhao
Pages: 1995-2003
Published online: 14 Jul 2022
AbstractforDiscovery of novel mRNA demethylase FTO inhibitors against esophageal cancer | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
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Article
Discovery of benzochalcone derivative as a potential antigastric cancer agent targeting signal transducer and activator of transcription 3 (STAT3)
Jinyun Dong, Jing Yang, Wenkai Yu, Haobin Li, Maohua Cai, Jing-Li Xu, Han-Dong Xu, Yun-Fu Shi, Xiaoqing Guan, Xiang‑Dong Cheng & Jiang‑Jiang Qin
Pages: 2004-2016
Published online: 18 Jul 2022
AbstractforDiscovery of benzochalcone derivative as a potential antigastric cancer agent targeting signal transducer and activator of transcription 3 (STAT3) | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
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Article
Discovery and SAR analysis of phenylbenzo[d][1,3]dioxole-based proprotein convertase subtilisin/kexin type 9 inhibitors
Fahui Li, Lihui Zhang, Jinhong Feng & Lei Zhang
Pages: 2017-2035
Published online: 19 Jul 2022
AbstractforDiscovery and SAR analysis of phenylbenzo[d][1,3]dioxole-based proprotein convertase subtilisin/kexin type 9 inhibitors | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
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Review

Review
The old world salsola as a source of valuable secondary metabolites endowed with diverse pharmacological activities: a review
Mai H. ElNaggar, Wagdy M. Eldehna, Mohammed A. S. Abourehab & Fatma M. Abdel Bar
Pages: 2036-2062
Published online: 25 Jul 2022
AbstractforThe old world salsola as a source of valuable secondary metabolites endowed with diverse pharmacological activities: a review | Full Text | References | PDF (3.9 MB) | EPUB
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Research Papers

Article
Benzoxazole derivatives as new VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, in silico studies, and antiproliferative evaluation
Mohammed S. Taghour, Hazem A. Mahdy, Maher H. Gomaa, Ahmed Aglan, Mahmoud Gomaa Eldeib, Alaa Elwan, Mohammed A. Dahab, Eslam B. Elkaeed, Aisha A. Alsfouk, Mohamed M. Khalifa, Ibrahim H. Eissa & Hazem Elkady
Pages: 2063-2077
Published online: 25 Jul 2022
AbstractforBenzoxazole derivatives as new VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, in silico studies, and antiproliferative evaluation | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
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Article
Design, synthesis, biological evaluation and molecular docking studies of novel pleuromutilin derivatives containing nitrogen heterocycle and alkylamine groups
Qi Wang, Jie Liu, Zi-Dan Zhou, Ke-Xin Zhou, Fei Li, Qi-Wen Zhang, Shou-Kai Wang, Wei Wang, Zhen Jin & You-Zhi Tang
Pages: 2078-2091
Published online: 25 Jul 2022
AbstractforDesign, synthesis, biological evaluation and molecular docking studies of novel pleuromutilin derivatives containing nitrogen heterocycle and alkylamine groups | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
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Article
The gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth
Viviana De Luca, Vincenzo Carginale, Claudiu T. Supuran & Clemente Capasso
Pages: 2092-2098
Published online: 28 Jul 2022
AbstractforThe gram-negative bacterium Escherichia coli as a model for testing the effect of carbonic anhydrase inhibition on bacterial growth | Full Text | References | PDF (1.5 MB)
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Brief Report

Brief Report
Fluorosulfate-containing pyrazole heterocycles as selective BuChE inhibitors: structure-activity relationship and biological evaluation for the treatment of Alzheimer’s disease
Huan-Huan Li, Chengyao Wu, Shi-Long Zhang, Jian-Guo Yang, Hua-Li Qin & Wenjian Tang
Pages: 2099-2111
Published online: 28 Jul 2022
AbstractforFluorosulfate-containing pyrazole heterocycles as selective BuChE inhibitors: structure-activity relationship and biological evaluation for the treatment of Alzheimer’s disease | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Research Papers

Article
Ligand-based design, synthesis, computational insights, and in vitro studies of novel N-(5-Nitrothiazol-2-yl)-carboxamido derivatives as potent inhibitors of SARS-CoV-2 main protease
Mohamed Elagawany, Ayman Abo Elmaaty, Ahmed Mostafa, Noura M. Abo Shama, Eman Y. Santali, Bahaa Elgendy & Ahmed A. Al-Karmalawy
Pages: 2112-2132
Published online: 31 Jul 2022
AbstractforLigand-based design, synthesis, computational insights, and in vitro studies of novel N-(5-Nitrothiazol-2-yl)-carboxamido derivatives as potent inhibitors of SARS-CoV-2 main protease | Full Text | References | PDF (5.9 MB) | EPUB | Supplemental
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Article
Targeting p21-activated kinase 4 (PAK4) with pyrazolo[3,4-d]pyrimidine derivative SPA7012 attenuates hepatic ischaemia-reperfusion injury in mice
Yuancheng Mao, Eun Lee, Xiaohui Yang, Eun Ju Bae, Raok Jeon & Byung-Hyun Park
Pages: 2133-2146
Published online: 03 Aug 2022
AbstractforTargeting p21-activated kinase 4 (PAK4) with pyrazolo[3,4-d]pyrimidine derivative SPA7012 attenuates hepatic ischaemia-reperfusion injury in mice | Full Text | References | PDF (3.2 MB) | EPUB
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Article
3-Arylcoumarin inhibits vascular calcification by inhibiting the generation of AGEs and anti-oxidative stress
YuFei Li, Yinbo Pan, Liying Wang, Xiaojing Wang, Haiping Chu, Yan Li, Jie Sun & Yanling Mu
Pages: 2147-2157
Published online: 11 Aug 2022
Abstractfor3-Arylcoumarin inhibits vascular calcification by inhibiting the generation of AGEs and anti-oxidative stress | Full Text | References | PDF (2.9 MB) | EPUB
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Article
Zinc pyrithione is a potent inhibitor of PLPro and cathepsin L enzymes with ex vivo inhibition of SARS-CoV-2 entry and replication
Jerneja Kladnik, Ana Dolinar, Jakob Kljun, David Perea, Judith Grau-Expósito, Meritxell Genescà, Marko Novinec, Maria J. Buzon & Iztok Turel
Pages: 2158-2168
Published online: 09 Aug 2022
AbstractforZinc pyrithione is a potent inhibitor of PLPro and cathepsin L enzymes with ex vivo inhibition of SARS-CoV-2 entry and replication | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
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Review

Review
A new era for the design of TRPV1 antagonists and agonists with the use of structural information and molecular docking of capsaicin-like compounds
Julio Caballero
Pages: 2169-2178
Published online: 16 Aug 2022
AbstractforA new era for the design of TRPV1 antagonists and agonists with the use of structural information and molecular docking of capsaicin-like compounds | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Research Papers

Article
Structure-guided approach on the role of substitution on amide-linked bipyrazoles and its effect on their anti-inflammatory activity
Souraya A. Domiati, Khaled H. Abd El Galil, Mohammed A. S. Abourehab, Tamer M. Ibrahim & Hanan M. Ragab
Pages: 2179-2190
Published online: 11 Aug 2022
AbstractforStructure-guided approach on the role of substitution on amide-linked bipyrazoles and its effect on their anti-inflammatory activity | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1146 Views
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Article
New quinoline and isatin derivatives as apoptotic VEGFR-2 inhibitors: design, synthesis, anti-proliferative activity, docking, ADMET, toxicity, and MD simulation studies
Eslam B. Elkaeed, Mohammed S. Taghour, Hazem A. Mahdy, Wagdy M. Eldehna, Nehal M. El-Deeb, Ahmed M. Kenawy, Bshra A. Alsfouk, Mohammed A. Dahab, Ahmed M. Metwaly, Ibrahim H. Eissa & Mohamed A. El-Zahabi
Pages: 2191-2205
Published online: 16 Aug 2022
AbstractforNew quinoline and isatin derivatives as apoptotic VEGFR-2 inhibitors: design, synthesis, anti-proliferative activity, docking, ADMET, toxicity, and MD simulation studies | Full Text | References | PDF (4.7 MB) | EPUB | Supplemental
  • 2250 Views
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Article
Anti-cancer and immunomodulatory evaluation of new nicotinamide derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: in vitro and in silico studies
Reda G. Yousef, Alaa Elwan, Ibraheem M. M. Gobaara, Ahmed B. M. Mehany, Wagdy M. Eldehna, Souad A. El-Metwally, Bshra A. Alsfouk, Eslam B. Elkaeed, Ahmed M. Metwaly & Ibrahim H. Eissa
Pages: 2206-2222
Published online: 18 Aug 2022
AbstractforAnti-cancer and immunomodulatory evaluation of new nicotinamide derivatives as potential VEGFR-2 inhibitors and apoptosis inducers: in vitro and in silico studies | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
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Article
Design, synthesis, and biological screening of a series of 4′-fluoro-benzotriazole-acrylonitrile derivatives as microtubule-destabilising agents (MDAs)
Federico Riu, Roberta Ibba, Stefano Zoroddu, Simona Sestito, Michele Lai, Sandra Piras, Luca Sanna, Valentina Bordoni, Luigi Bagella & Antonio Carta
Pages: 2223-2240
Published online: 17 Aug 2022
AbstractforDesign, synthesis, and biological screening of a series of 4′-fluoro-benzotriazole-acrylonitrile derivatives as microtubule-destabilising agents (MDAs) | Full Text | References | PDF (4 MB) | EPUB | Supplemental
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Article
Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs
Qiaohua Qin, Ruifeng Wang, Qinglin Fu, Guoqi Zhang, Tianxiao Wu, Nian Liu, Ruicheng Lv, Wenbo Yin, Yin Sun, Yixiang Sun, Dongmei Zhao & Maosheng Cheng
Pages: 2241-2255
Published online: 17 Aug 2022
AbstractforDesign, synthesis, and biological evaluation of potent FAK-degrading PROTACs | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Article
Enaminone-based carboxylic acids as novel non-classical carbonic anhydrases inhibitors: design, synthesis and in vitro biological assessment
Mahmoud F. Abo-Ashour, Hadia Almahli, Alessandro Bonardi, Amira Khalil, Tarfah Al-Warhi, Sara T. Al-Rashood, Hatem A. Abdel-Aziz, Alessio Nocentini, Claudiu T. Supuran & Wagdy M. Eldehna
Pages: 2256-2264
Published online: 23 Aug 2022
AbstractforEnaminone-based carboxylic acids as novel non-classical carbonic anhydrases inhibitors: design, synthesis and in vitro biological assessment | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
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Article
Discovery of novel thiazolyl-pyrazolines as dual EGFR and VEGFR-2 inhibitors endowed with in vitro antitumor activity towards non-small lung cancer
Esraa A. Abdelsalam, Amer Ali Abd El-Hafeez, Wagdy M. Eldehna, Mahmoud A. El Hassab, Hala Mohamed M. Marzouk, Mahmoud M. Elaasser, Nageh A. Abou Taleb, Kamilia M. Amin, Hatem A. Abdel-Aziz, Pradipta Ghosh & Sherif F. Hammad
Pages: 2265-2282
Published online: 23 Aug 2022
AbstractforDiscovery of novel thiazolyl-pyrazolines as dual EGFR and VEGFR-2 inhibitors endowed with in vitro antitumor activity towards non-small lung cancer | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
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Article
Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M
Ahmed A. Gaber, Mohamed Sobhy, Abdallah Turky, Hanan Gaber Abdulwahab, Ahmed A. Al-Karmalawy, Mostafa. A. Elhendawy, Mohamed. M. Radwan, Eslam B. Elkaeed, Ibrahim M. Ibrahim, Heba S. A. Elzahabi & Ibrahim H. Eissa
Pages: 2283-2303
Published online: 23 Aug 2022
AbstractforDiscovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
  • 1978 Views
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Review

Review
Research progress on the synthesis and pharmacology of 1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives: a mini review
Jing-Jing Wang, Wen Sun, Wei-Dong Jia, Ming Bian & Li-Jun Yu
Pages: 2304-2319
Published online: 23 Aug 2022
AbstractforResearch progress on the synthesis and pharmacology of 1,3,4-oxadiazole and 1,2,4-oxadiazole derivatives: a mini review | Full Text | References | PDF (2.2 MB) | EPUB
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Research Papers

Article
New pyrazolylpyrazoline derivatives as dual acting antimalarial-antileishamanial agents: synthesis, biological evaluation and molecular modelling simulations
Adnan A. Bekhit, Eskedar T. Lodebo, Ariaya Hymete, Hanan M. Ragab, Salma A. Bekhit, Kikuko Amagase, Afnan Batubara, Mohammed A. S. Abourehab, Alaa El-Din A. Bekhit & Tamer M. Ibrahim
Pages: 2320-2333
Published online: 29 Aug 2022
AbstractforNew pyrazolylpyrazoline derivatives as dual acting antimalarial-antileishamanial agents: synthesis, biological evaluation and molecular modelling simulations | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1409 Views
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Article
Discovery of novel conjugates of quinoline and thiazolidinone urea as potential anti-colorectal cancer agent
Li Xiong, Huan He, Mengmeng Fan, Liping Hu, Fei Wang, Xiaomeng Song, Shengmin Shi & Baohui Qi
Pages: 2334-2347
Published online: 31 Aug 2022
AbstractforDiscovery of novel conjugates of quinoline and thiazolidinone urea as potential anti-colorectal cancer agent | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1144 Views
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Article
Multitarget drugs as potential therapeutic agents for alzheimer’s disease. A new family of 5-substituted indazole derivatives as cholinergic and BACE1 inhibitors
Pedro González-Naranjo, Concepción Pérez, Marina González-Sánchez, Adrián Gironda-Martínez, Eugenia Ulzurrun, Fernando Bartolomé, Marcos Rubio-Fernández, Angeles Martin-Requero, Nuria E. Campillo & Juan A. Páez
Pages: 2348-2356
Published online: 01 Sep 2022
AbstractforMultitarget drugs as potential therapeutic agents for alzheimer’s disease. A new family of 5-substituted indazole derivatives as cholinergic and BACE1 inhibitors | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 1439 Views
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Article
Rational design, synthesis, and pharmacological characterisation of dicarbonyl curcuminoid analogues with improved stability against lung cancer via ROS and ER stress mediated cell apoptosis and pyroptosis
Tao Wei, Zhiwei Zheng, Xiaoyan Wei, Yugang Liu, Wentao Li, Bingqing Fang, Di Yun, Zhaojun Dong, Baozhu Yi, Wulan Li, Xiaoping Wu, Dezhi Chen, Liping Chen & Jianzhang Wu
Pages: 2357-2369
Published online: 29 Aug 2022
AbstractforRational design, synthesis, and pharmacological characterisation of dicarbonyl curcuminoid analogues with improved stability against lung cancer via ROS and ER stress mediated cell apoptosis and pyroptosis | Full Text | References | PDF (2.5 MB) | EPUB
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Article
Upregulation of p53 through induction of MDM2 degradation: improved potency through the introduction of an alkylketone sidechain on the anthraquinone core
Ravi Tripathi, Abiodun Anifowose, Wen Lu, Xiaoxiao Yang & Binghe Wang
Pages: 2370-2381
Published online: 31 Aug 2022
AbstractforUpregulation of p53 through induction of MDM2 degradation: improved potency through the introduction of an alkylketone sidechain on the anthraquinone core | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Article
Synthesis and biological activity evaluation of 3-(hetero) arylideneindolin-2-ones as potential c-Src inhibitors
Salvatore Princiotto, Loana Musso, Fabrizio Manetti, Valentina Marcellini, Giovanni Maga, Emmanuele Crespan, Cecilia Perini, Nadia Zaffaroni, Giovanni Luca Beretta & Sabrina Dallavalle
Pages: 2382-2394
Published online: 01 Sep 2022
AbstractforSynthesis and biological activity evaluation of 3-(hetero) arylideneindolin-2-ones as potential c-Src inhibitors | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Brief Report

Brief Report
A hybrid of 1-deoxynojirimycin and benzotriazole induces preferential inhibition of butyrylcholinesterase (BuChE) over acetylcholinesterase (AChE)
Tereza Cristina Santos Evangelista, Óscar López, Adrián Puerta, Miguel X. Fernandes, Sabrina Baptista Ferreira, José M. Padrón, José G. Fernández-Bolaños, Magne O. Sydnes & Emil Lindbäck
Pages: 2395-2402
Published online: 06 Sep 2022
AbstractforA hybrid of 1-deoxynojirimycin and benzotriazole induces preferential inhibition of butyrylcholinesterase (BuChE) over acetylcholinesterase (AChE) | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
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Research Papers

Article
Novel hydroxyl carboximates derived from β-elemene: design, synthesis and anti-tumour activities evaluation
Yuan Gao, Nian-Dong Mao, Hao Che, Li Xu, Renren Bai, Li-Wei Wang, Xiang-Yang Ye & Tian Xie
Pages: 2403-2416
Published online: 06 Sep 2022
AbstractforNovel hydroxyl carboximates derived from β-elemene: design, synthesis and anti-tumour activities evaluation | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
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Article
Inhibition studies of the protozoan α-carbonic anhydrase from Trypanosoma cruzi with phenols
Alessandro Bonardi, Seppo Parkkila & Claudiu T. Supuran
Pages: 2417-2422
Published online: 06 Sep 2022
AbstractforInhibition studies of the protozoan α-carbonic anhydrase from Trypanosoma cruzi with phenols | Full Text | References | PDF (1.7 MB)
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Article
Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents
Jichao Chen, Yiping Duan, Xiaoxuan Yu, Jiarou Zhong, Jing Bai, Nian-Guang Li, Zheying Zhu & Jinyi Xu
Pages: 2423-2433
Published online: 06 Sep 2022
AbstractforDevelopment of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Article
Identification of novel pyrrolopyrimidine and pyrrolopyridine derivatives as potent ENPP1 inhibitors
Hee Jin Jeong, Hye Lim Lee, Sung Joon Kim, Jeong Hyun Jeong, Su Hyun Ji, Han Byeol Kim, Miso Kang, Hwan Won Chung, Chan Sun Park, Hyunah Choo, Hyo Jae Yoon, Nam-Jung Kim, Duck-Hyung Lee, Sanghee Lee & Seo-Jung Han
Pages: 2434-2451
Published online: 07 Sep 2022
AbstractforIdentification of novel pyrrolopyrimidine and pyrrolopyridine derivatives as potent ENPP1 inhibitors | Full Text | References | PDF (2.3 MB) | Supplemental
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Reviews

Review
Arctigenin: pharmacology, total synthesis, and progress in structure modification
Dan Wu, Lili Jin, Xing Huang, Hao Deng, Qing-kun Shen, Zhe-shan Quan, Changhao Zhang & Hong-Yan Guo
Pages: 2452-2477
Published online: 12 Sep 2022
AbstractforArctigenin: pharmacology, total synthesis, and progress in structure modification | Full Text | References | PDF (3.9 MB) | EPUB
  • 1993 Views
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Review
Anti-obesity carbonic anhydrase inhibitors: challenges and opportunities
Claudiu T. Supuran
Pages: 2478-2488
Published online: 08 Sep 2022
AbstractforAnti-obesity carbonic anhydrase inhibitors: challenges and opportunities | Full Text | References | PDF (2.2 MB)
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Research Papers

Article
Discovery of new symmetrical and asymmetrical nitrile-containing 1,4-dihydropyridine derivatives as dual kinases and P-glycoprotein inhibitors: synthesis, in vitro assays, and in silico studies
Mohamed H. Saad, Tarek F. El-Moselhy, Nabaweya S, El-Din, Ahmed B. M. Mehany, Amany Belal, Mohammed A. S. Abourehab, Haytham O. Tawfik & Mervat H. El-Hamamsy
Pages: 2489-2511
Published online: 12 Sep 2022
AbstractforDiscovery of new symmetrical and asymmetrical nitrile-containing 1,4-dihydropyridine derivatives as dual kinases and P-glycoprotein inhibitors: synthesis, in vitro assays, and in silico studies | Full Text | References | PDF (5.2 MB) | EPUB | Supplemental
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Article
Design, synthesis and biological evaluation of 2,4-pyrimidinediamine derivatives as ALK and HDACs dual inhibitors for the treatment of ALK addicted cancer
Dafeng Guo, Yu Yu, Binyu Long, Ping Deng, Dongzhi Ran, Lei Han, Jiecheng Zheng & Zongjie Gan
Pages: 2512-2529
Published online: 13 Sep 2022
AbstractforDesign, synthesis and biological evaluation of 2,4-pyrimidinediamine derivatives as ALK and HDACs dual inhibitors for the treatment of ALK addicted cancer | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
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Brief Report

Brief Report
Synthesis and antitumor activity of litseaone B analogues as tubulin polymerisation inhibitors
Wei Yang, Huining Peng, Yong Huang, Zhiyun Peng & Guangcheng Wang
Pages: 2530-2539
Published online: 13 Sep 2022
AbstractforSynthesis and antitumor activity of litseaone B analogues as tubulin polymerisation inhibitors | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Research Paper

Article
TiO2 nanotube immobilised 5-lipoxygenase-mediated screening and isolation of anti-inflammatory active compounds from the leaves of lonicera japonica thunb
Jinhua Zhu, Danyang Zhou, Dandan Wu, Wei Liu & Xiuhua Liu
Pages: 2540-2550
Published online: 19 Sep 2022
AbstractforTiO2 nanotube immobilised 5-lipoxygenase-mediated screening and isolation of anti-inflammatory active compounds from the leaves of lonicera japonica thunb | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Brief Report

Brief Report
Design, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors
Man Yang, Chenyao Li, Yajing Li, Chen Cheng, Meiyun Shi, Lei Yin, Hongyu Xue & Yajun Liu
Pages: 2551-2565
Published online: 19 Sep 2022
AbstractforDesign, synthesis, biological evaluation and molecular docking study of 2,4-diarylimidazoles and 2,4-bis(benzyloxy)-5-arylpyrimidines as novel HSP90 N-terminal inhibitors | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
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Research Paper

Article
Inhibitory prodrug mechanism for cysteine cathepsin-targeted self-controlled drug release
Floris J. van Dalen & Martijn Verdoes
Pages: 2566-2573
Published online: 19 Sep 2022
AbstractforInhibitory prodrug mechanism for cysteine cathepsin-targeted self-controlled drug release | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Correction

Correction
Correction
Page: 2574
Published online: 20 Sep 2022
CitationforCorrection | Full Text | PDF (382.9 KB) | EPUB
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Research Paper

Article
Design, synthesis and evaluation of novel small molecules acting as Keap1-Nrf2 protein-protein interaction inhibitors
Yunfeng Sun, Lulu Zheng, Bo Yang, Shuyu Ge, Qiang Li, Mingwan Zhang, Shenghui Shen & Yin Ying
Pages: 2575-2588
Published online: 21 Sep 2022
AbstractforDesign, synthesis and evaluation of novel small molecules acting as Keap1-Nrf2 protein-protein interaction inhibitors | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
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Brief Report

Brief Report
Novel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo
Yun Xiao, Yaoyao Yan, Juncheng Du, Xiaoxiao Feng, Famin Zhang, Xu Han, Yong Hu & Xinhua Liu
Pages: 2589-2597
Published online: 21 Sep 2022
AbstractforNovel 2-phenyl-4H-chromen derivatives: synthesis and anti-inflammatory activity evaluation in vitro and in vivo | Full Text | References | PDF (2.5 MB) | EPUB
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Research Papers

Article
The mechanism and pharmacodynamics of 2-((1H-indol-3-yl)thio/sulfinyl)-N-pheny acetamide derivative as a novel inhibitor against human respiratory syncytial virus
Ningning Cheng, Nan Jiang, Yuanhui Fu, Zhuxin Xu, Xianglei Peng, Jiemei Yu, Shan Cen, Yucheng Wang, Guoning Zhang, Yanpeng Zheng & Jinsheng He
Pages: 2598-2604
Published online: 21 Sep 2022
AbstractforThe mechanism and pharmacodynamics of 2-((1H-indol-3-yl)thio/sulfinyl)-N-pheny acetamide derivative as a novel inhibitor against human respiratory syncytial virus | Full Text | References | PDF (2.6 MB) | EPUB
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Article
Privileged multi-target directed propargyl-tacrines combining cholinesterase and monoamine oxidase inhibition activities
Zofia Chrienova, Eugenie Nepovimova, Rudolf Andrys, Rafael Dolezal, Jana Janockova, Lubica Muckova, Lenka Fabova, Ondrej Soukup, Patrik Oleksak, Martin Valis, Jan Korabecny, José Marco-Contelles & Kamil Kuca
Pages: 2605-2620
Published online: 21 Sep 2022
AbstractforPrivileged multi-target directed propargyl-tacrines combining cholinesterase and monoamine oxidase inhibition activities | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Article
Inhibition of Toxoplasma gondii by 1,2,4-triazole-based compounds: marked improvement in selectivity relative to the standard therapy pyrimethamine and sulfadiazine
Lidia Węglińska, Adrian Bekier, Nazar Trotsko, Barbara Kaproń, Tomasz Plech, Katarzyna Dzitko & Agata Paneth
Pages: 2621-2634
Published online: 27 Sep 2022
AbstractforInhibition of Toxoplasma gondii by 1,2,4-triazole-based compounds: marked improvement in selectivity relative to the standard therapy pyrimethamine and sulfadiazine | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Article
Design and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII
Tarfah Al-Warhi, Mostafa M. Elbadawi, Alessandro Bonardi, Alessio Nocentini, Ahmed A. Al-Karmalawy, Nada Aljaeed, Ohoud J. Alotaibi, Hatem A. Abdel-Aziz, Claudiu T. Supuran & Wagdy M. Eldehna
Pages: 2635-2643
Published online: 22 Sep 2022
AbstractforDesign and synthesis of benzothiazole-based SLC-0111 analogues as new inhibitors for the cancer-associated carbonic anhydrase isoforms IX and XII | Full Text | References | PDF (1.6 MB) | Supplemental
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Article
Design and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity
Amr Sonousi, Rasha A. Hassan, Eman O. Osman, Amr M. Abdou & Soha H. Emam
Pages: 2644-2659
Published online: 22 Sep 2022
AbstractforDesign and synthesis of novel quinazolinone-based derivatives as EGFR inhibitors with antitumor activity | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Article
Design and synthesis of new indole drug candidates to treat Alzheimer’s disease and targeting neuro-inflammation using a multi-target-directed ligand (MTDL) strategy
Phoebe F. Lamie, Maha M. Abdel-Fattah & John N. Philoppes
Pages: 2660-2678
Published online: 22 Sep 2022
AbstractforDesign and synthesis of new indole drug candidates to treat Alzheimer’s disease and targeting neuro-inflammation using a multi-target-directed ligand (MTDL) strategy | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
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Article
Design and synthesis of new trimethoxylphenyl-linked combretastatin analogues loaded on diamond nanoparticles as a panel for ameliorated solubility and antiproliferative activity
Islam Zaki, Amal M. Y. Moustafa, Botros Y. Beshay, Reham E. Masoud, Mohammed A. I. Elbastawesy, Mohammed A. S. Abourehab & Mohamed Y. Zakaria
Pages: 2679-2701
Published online: 26 Sep 2022
AbstractforDesign and synthesis of new trimethoxylphenyl-linked combretastatin analogues loaded on diamond nanoparticles as a panel for ameliorated solubility and antiproliferative activity | Full Text | References | PDF (4.7 MB) | EPUB | Supplemental
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Article
Design and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes
Mazin A. A. Najm, Walaa R. Mahmoud, Azza T. Taher, Safinaz E-S. Abbas, Fadi M. Awadallah, Heba Abdelrasheed Allam, Daniela Vullo & Claudiu T. Supuran
Pages: 2702-2709
Published online: 27 Sep 2022
AbstractforDesign and synthesis of some new benzoylthioureido phenyl derivatives targeting carbonic anhydrase enzymes | Full Text | References | PDF (1.1 MB) | EPUB | Supplemental
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Article
Molecular design, synthesis and biological evaluation of novel 1,2,5-trisubstituted benzimidazole derivatives as cytotoxic agents endowed with ABCB1 inhibitory action to overcome multidrug resistance in cancer cells
Abeer H. A. Abdelhafiz, Rabah A. T. Serya, Deena S. Lasheen, Nessa Wang, Mansour Sobeh, Michael Wink & Khaled A. M. Abouzid
Pages: 2710-2724
Published online: 27 Sep 2022
AbstractforMolecular design, synthesis and biological evaluation of novel 1,2,5-trisubstituted benzimidazole derivatives as cytotoxic agents endowed with ABCB1 inhibitory action to overcome multidrug resistance in cancer cells | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
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Article
Novel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents
Juliusz Maksymilian Walczak, Dorota Iwaszkiewicz-Grześ, Michalina Ziomkowska, Magdalena Śliwka-Kaszyńska, Mateusz Daśko, Piotr Trzonkowski & Grzegorz Cholewiński
Pages: 2725-2741
Published online: 03 Oct 2022
AbstractforNovel amides of mycophenolic acid and some heterocyclic derivatives as immunosuppressive agents | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
  • 1247 Views
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Brief Report

Brief Report
Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors
Yaqing Zuo, Rongrong Li, Yan Zhang, Guochen Bao, Yi Le & Longjia Yan
Pages: 2742-2754
Published online: 29 Sep 2022
AbstractforDesign, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 1054 Views
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Research Papers

Article
Design, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors
Shanbo Yang, Chao Wang, Lingyu Shi, Jing Chang, Yujing Zhang, Jingsen Meng, Wenjing Liu, Jun Zeng, Renshuai Zhang, Yingchun Shao & Dongming Xing
Pages: 2755-2764
Published online: 05 Oct 2022
AbstractforDesign, synthesis and biological evaluation of novel diarylpyridine derivatives as tubulin polymerisation inhibitors | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 1040 Views
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Article
Dependence on linkers’ flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents
Haytham O. Tawfik, Amany Belal, Mohammed A. S. Abourehab, Andrea Angeli, Alessandro Bonardi, Claudiu T. Supuran & Mervat H. El-Hamamsy
Pages: 2765-2785
Published online: 09 Oct 2022
AbstractforDependence on linkers’ flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
  • 1310 Views
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Brief Report

Brief Report
Activation studies with amino acids and amines of a β-carbonic anhydrase from Mammaliicoccus (Staphylococcus) sciuri previously annotated as Staphylococcus aureus (SauBCA) carbonic anhydrase
Andrea Angeli, Linda J Urbański, Clemente Capasso, Seppo Parkkila & Claudiu T. Supuran
Pages: 2786-2792
Published online: 09 Oct 2022
AbstractforActivation studies with amino acids and amines of a β-carbonic anhydrase from Mammaliicoccus (Staphylococcus) sciuri previously annotated as Staphylococcus aureus (SauBCA) carbonic anhydrase | Full Text | References | PDF (1.2 MB)
  • 937 Views
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Correction

Correction
Correction
Pages: 2793-2794
Published online: 13 Oct 2022
CitationforCorrection | Full Text | PDF (285.7 KB) | EPUB
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