Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 36, Issue 1 (2021)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 36, Issue 1 (2021)

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Article
HT-SuMD: making molecular dynamics simulations suitable for fragment-based screening. A comparative study with NMR
Francesca Ferrari, Maicol Bissaro, Simone Fabbian, Jessica De Almeida Roger, Stefano Mammi, Stefano Moro, Massimo Bellanda & Mattia Sturlese
Pages: 1-14
Published online: 28 Oct 2020
AbstractforHT-SuMD: making molecular dynamics simulations suitable for fragment-based screening. A comparative study with NMR | Full Text | References | PDF (3 MB) | EPUB | Supplemental
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Article
Pharmacophore-based virtual screening, synthesis, biological evaluation, and molecular docking study of novel pyrrolizines bearing urea/thiourea moieties with potential cytotoxicity and CDK inhibitory activities
Ahmed M. Shawky, Nashwa A. Ibrahim, Mohammed A. S. Abourehab, Ashraf N. Abdalla & Ahmed M. Gouda
Pages: 15-33
Published online: 26 Oct 2020
AbstractforPharmacophore-based virtual screening, synthesis, biological evaluation, and molecular docking study of novel pyrrolizines bearing urea/thiourea moieties with potential cytotoxicity and CDK inhibitory activities | Full Text | References | PDF (4.3 MB) | EPUB | Supplemental
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Brief Report
Identification of histone deacetylase inhibitors with (arylidene)aminoxy scaffold active in uveal melanoma cell lines
Susanna Nencetti, Doretta Cuffaro, Elisa Nuti, Lidia Ciccone, Armando Rossello, Marina Fabbi, Flavio Ballante, Gabriella Ortore, Grazia Carbotti, Francesco Campelli, Irene Banti, Rosaria Gangemi, Garland R. Marshall & Elisabetta Orlandini
Pages: 34-47
Published online: 26 Oct 2020
AbstractforIdentification of histone deacetylase inhibitors with (arylidene)aminoxy scaffold active in uveal melanoma cell lines | Full Text | References | PDF (3.5 MB) | Supplemental
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Article
Activation of carbonic anhydrases from human brain by amino alcohol oxime ethers: towards human carbonic anhydrase VII selective activators
Alessio Nocentini, Doretta Cuffaro, Lidia Ciccone, Elisabetta Orlandini, Susanna Nencetti, Elisa Nuti, Armando Rossello & Claudiu T. Supuran
Pages: 48-57
Published online: 25 Oct 2020
AbstractforActivation of carbonic anhydrases from human brain by amino alcohol oxime ethers: towards human carbonic anhydrase VII selective activators | Full Text | References | PDF (2.8 MB)
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Article
Synthesis and evaluation of anticancer activities of 2- or 4-substituted 3-(N-benzyltriazolylmethyl)-13α-oestrone derivatives
Rebeka Jójárt, Seyyed Ashkan Senobar Tahaei, Péter Trungel-Nagy, Zoltán Kele, Renáta Minorics, Gábor Paragi, István Zupkó & Erzsébet Mernyák
Pages: 58-67
Published online: 29 Oct 2020
AbstractforSynthesis and evaluation of anticancer activities of 2- or 4-substituted 3-(N-benzyltriazolylmethyl)-13α-oestrone derivatives | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 1960 Views
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Article
Lipoprotein-associated phospholipase A2 (Lp-PLA2) – possible diagnostic and risk biomarker in chronic ischaemic heart disease
Adriana Diaconu, Bogdan-Ioan Coculescu, Gheorghe Manole, Horațiu Vultur, Elena Claudia Coculescu, Cristina Maria Stocheci, Ioan-Sorin Tudorache, Alexandra-Ligia Dincă & Valeriu Gabi Dincă
Pages: 68-73
Published online: 13 Nov 2020
AbstractforLipoprotein-associated phospholipase A2 (Lp-PLA2) – possible diagnostic and risk biomarker in chronic ischaemic heart disease | Full Text | References | PDF (1.4 MB) | EPUB
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Article
Effect of 3-subsitution of quinolinehydroxamic acids on selectivity of histone deacetylase isoforms
Samir Mehndiratta, Mei-Chuan Chen, Yuh-Hsuan Chao, Cheng-Hsin Lee, Jing-Ping Liou, Mei-Jung Lai & Hsueh-Yun Lee
Pages: 74-84
Published online: 08 Nov 2020
AbstractforEffect of 3-subsitution of quinolinehydroxamic acids on selectivity of histone deacetylase isoforms | Full Text | References | PDF (1.9 MB) | Supplemental
  • 2201 Views
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Brief Report
The SNAP-tag technology revised: an effective chemo-enzymatic approach by using a universal azide-based substrate
Rosa Merlo, Diego Caprioglio, Michele Cillo, Anna Valenti, Rosanna Mattossovich, Castrese Morrone, Alberto Massarotti, Franca Rossi, Riccardo Miggiano, Antonio Leonardi, Alberto Minassi & Giuseppe Perugino
Pages: 85-97
Published online: 29 Oct 2020
AbstractforThe SNAP-tag technology revised: an effective chemo-enzymatic approach by using a universal azide-based substrate | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Article
Identification of a dual TAOK1 and MAP4K5 inhibitor using a structure-based virtual screening approach
Min-Wu Chao, Tony Eight Lin, Wei-Chun HuangFu, Chao-Di Chang, Huang-Ju Tu, Liang-Chieh Chen, Shih-Chung Yen, Tzu-Ying Sung, Wei-Jan Huang, Chia-Ron Yang, Shiow-Lin Pan & Kai-Cheng Hsu
Pages: 98-108
Published online: 09 Nov 2020
AbstractforIdentification of a dual TAOK1 and MAP4K5 inhibitor using a structure-based virtual screening approach | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
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Article
Inhibitory evaluation of Curculigo latifolia on α-glucosidase, DPP (IV) and in vitro studies in antidiabetic with molecular docking relevance to type 2 diabetes mellitus
Nur Athirah Zabidi, Nur Akmal Ishak, Muhajir Hamid, Siti Efliza Ashari & Muhammad Alif Mohammad Latif
Pages: 109-121
Published online: 29 Nov 2020
AbstractforInhibitory evaluation of Curculigo latifolia on α-glucosidase, DPP (IV) and in vitro studies in antidiabetic with molecular docking relevance to type 2 diabetes mellitus | Full Text | References | PDF (2.1 MB) | EPUB
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Article
Differences in the efficiency of 3-deazathiamine and oxythiamine pyrophosphates as inhibitors of pyruvate dehydrogenase complex and growth of HeLa cells in vitro
Ewa Grabowska, Magdalena Czerniecka, Urszula Czyżewska, Aneta Zambrzycka, Zenon Łotowski & Adam Tylicki
Pages: 122-129
Published online: 13 Nov 2020
AbstractforDifferences in the efficiency of 3-deazathiamine and oxythiamine pyrophosphates as inhibitors of pyruvate dehydrogenase complex and growth of HeLa cells in vitro | Full Text | References | PDF (2 MB) | EPUB
  • 1927 Views
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Brief Report
Analogues of 2′-hydroxychalcone with modified C4-substituents as the inhibitors against human acetylcholinesterase
Sri Devi Sukumaran, Shah Bakhtiar Nasir, Jia Ti Tee, Michael J. C. Buckle, Rozana Othman, Noorsaadah Abd. Rahman, Vannajan Sanghiran Lee, Syed Nasir Abbas Bukhari & Chin Fei Chee
Pages: 130-137
Published online: 26 Nov 2020
AbstractforAnalogues of 2′-hydroxychalcone with modified C4-substituents as the inhibitors against human acetylcholinesterase | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2321 Views
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Brief Report
Tuning the activity of iminosugars: novel N-alkylated deoxynojirimycin derivatives as strong BuChE inhibitors
Ana I. Ahuja-Casarín, Penélope Merino-Montiel, José Luis Vega-Baez, Sara Montiel-Smith, Miguel X. Fernandes, Irene Lagunes, Inés Maya, José M. Padrón, Óscar López & José G. Fernández-Bolaños
Pages: 138-146
Published online: 23 Nov 2020
AbstractforTuning the activity of iminosugars: novel N-alkylated deoxynojirimycin derivatives as strong BuChE inhibitors | Full Text | References | PDF (1.5 MB) | Supplemental
  • 2931 Views
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Article
Repurposing existing drugs: identification of SARS-CoV-2 3C-like protease inhibitors
Wei-Chung Chiou, Meng-Shiuan Hsu, Yun-Ti Chen, Jinn-Moon Yang, Yeou-Guang Tsay, Hsiu-Chen Huang & Cheng Huang
Pages: 147-153
Published online: 12 Jan 2021
AbstractforRepurposing existing drugs: identification of SARS-CoV-2 3C-like protease inhibitors | Full Text | References | PDF (1.4 MB) | EPUB
  • 5373 Views
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Article
Dammarane triterpenes targeting α-synuclein: biological activity and evaluation of binding sites by molecular docking
Alberto Cornejo, Julio Caballero, Mario Simirgiotis, Vanessa Torres, Luisa Sánchez, Nicolás Díaz, Marcela Guimaraes, Marcos Hernández, Carlos Areche, Sergio Alfaro, Leonardo Caballero & Francisco Melo
Pages: 154-162
Published online: 14 Dec 2020
AbstractforDammarane triterpenes targeting α-synuclein: biological activity and evaluation of binding sites by molecular docking | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
  • 3093 Views
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Article
Preclinical in vitro screening of newly synthesised amidino substituted benzimidazoles and benzothiazoles
Livio Racané, Maja Cindrić, Ivo Zlatar, Tatjana Kezele, Astrid Milić, Karmen Brajša & Marijana Hranjec
Pages: 163-174
Published online: 06 Jan 2021
AbstractforPreclinical in vitro screening of newly synthesised amidino substituted benzimidazoles and benzothiazoles | Full Text | References | PDF (2.1 MB) | EPUB
  • 2259 Views
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Article
Nanovesicles released by OKT3 hybridoma express fully active antibodies
Mariantonia Logozzi, Rossella Di Raimo, Francesca Properzi, Stefano Barca, Daniela F. Angelini, Davide Mizzoni, Mario Falchi, Luca Battistini & Stefano Fais
Pages: 175-182
Published online: 06 Jan 2021
AbstractforNanovesicles released by OKT3 hybridoma express fully active antibodies | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
  • 2528 Views
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Article
The insulin-degrading enzyme as a link between insulin and neuropeptides metabolism
Dorota Wacławczyk, Jerzy Silberring & Giuseppe Grasso
Pages: 183-187
Published online: 05 Jan 2021
AbstractforThe insulin-degrading enzyme as a link between insulin and neuropeptides metabolism | Full Text | References | PDF (863.8 KB) | EPUB
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Article
Morpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations
Rani Sasidharan, Bo Hyun Eom, Jeong Hyun Heo, Jong Eun Park, Mohamed A. Abdelgawad, Arafa Musa, Nicola Gambacorta, Orazio Nicolotti, Sreedharannair Leelabaiamma Manju, Bijo Mathew & Hoon Kim
Pages: 188-197
Published online: 12 Jan 2021
AbstractforMorpholine-based chalcones as dual-acting monoamine oxidase-B and acetylcholinesterase inhibitors: synthesis and biochemical investigations | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 3311 Views
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Article
Discovery of new non-pyrimidine scaffolds as Plasmodium falciparum DHFR inhibitors by fragment-based screening
Marie Hoarau, Jarunee Vanichtanankul, Nitipol Srimongkolpithak, Danoo Vitsupakorn, Yongyuth Yuthavong & Sumalee Kamchonwongpaisan
Pages: 198-206
Published online: 02 Feb 2021
AbstractforDiscovery of new non-pyrimidine scaffolds as Plasmodium falciparum DHFR inhibitors by fragment-based screening | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 2456 Views
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Article
Discovery of orally active chalcones as histone lysine specific demethylase 1 inhibitors for the treatment of leukaemia
Yang Li, Ying Sun, Yang Zhou, Xinyang Li, Huan Zhang & Guojun Zhang
Pages: 207-217
Published online: 13 Dec 2020
AbstractforDiscovery of orally active chalcones as histone lysine specific demethylase 1 inhibitors for the treatment of leukaemia | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 1879 Views
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Article
Synthesis of some quinazolinones inspired from the natural alkaloid L-norephedrine as EGFR inhibitors and radiosensitizers
Mostafa M. Ghorab, Maged S. Abdel-Kader, Ali S. Alqahtani & Aiten M. Soliman
Pages: 218-238
Published online: 28 Dec 2020
AbstractforSynthesis of some quinazolinones inspired from the natural alkaloid L-norephedrine as EGFR inhibitors and radiosensitizers | Full Text | References | PDF (4.3 MB) | EPUB | Supplemental
  • 2448 Views
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Article
New potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives
Olga Ciupak, Mateusz Daśko, Karol Biernacki, Janusz Rachon, Maciej Masłyk, Konrad Kubiński, Aleksandra Martyna & Sebastian Demkowicz
Pages: 239-248
Published online: 15 Dec 2020
AbstractforNew potent steroid sulphatase inhibitors based on 6-(1-phenyl-1H-1,2,3-triazol-4-yl)naphthalen-2-yl sulphamate derivatives | Full Text | References | PDF (1.9 MB) | EPUB
  • 2262 Views
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Article
Production, purification and biochemical characterisation of a novel lipase from a newly identified lipolytic bacterium Staphylococcus caprae NCU S6
Junxin Zhao, Maomao Ma, Zheling Zeng, Ping Yu, Deming Gong & Shuguang Deng
Pages: 249-257
Published online: 17 Dec 2020
AbstractforProduction, purification and biochemical characterisation of a novel lipase from a newly identified lipolytic bacterium Staphylococcus caprae NCU S6 | Full Text | References | PDF (1.5 MB) | EPUB
  • 6115 Views
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Article
Screening the dermatological potential of Plectranthus species components: antioxidant and inhibitory capacities over elastase, collagenase and tyrosinase
Joana M. Andrade, Eva María Domínguez-Martín, Marisa Nicolai, Célia Faustino, Luís Monteiro Rodrigues & Patrícia Rijo
Pages: 258-270
Published online: 15 Dec 2020
AbstractforScreening the dermatological potential of Plectranthus species components: antioxidant and inhibitory capacities over elastase, collagenase and tyrosinase | Full Text | References | PDF (2.8 MB) | EPUB
  • 3733 Views
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Article
Novel oxindole/benzofuran hybrids as potential dual CDK2/GSK-3β inhibitors targeting breast cancer: design, synthesis, biological evaluation, and in silico studies
Wagdy M. Eldehna, Sara T. Al-Rashood, Tarfah Al-Warhi, Razan O. Eskandrani, Amal Alharbi & Ahmed M. El Kerdawy
Pages: 271-286
Published online: 16 Dec 2020
AbstractforNovel oxindole/benzofuran hybrids as potential dual CDK2/GSK-3β inhibitors targeting breast cancer: design, synthesis, biological evaluation, and in silico studies | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
  • 4271 Views
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Article
Novel positive allosteric modulators of A2B adenosine receptor acting as bone mineralisation promoters
Elisabetta Barresi, Chiara Giacomelli, Laura Marchetti, Emma Baglini, Silvia Salerno, Giovanni Greco, Federico Da Settimo, Claudia Martini, Maria Letizia Trincavelli & Sabrina Taliani
Pages: 287-295
Published online: 17 Dec 2020
AbstractforNovel positive allosteric modulators of A2B adenosine receptor acting as bone mineralisation promoters | Full Text | References | PDF (2.1 MB) | EPUB
  • 1642 Views
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Article
Design, synthesis and evaluation of carbazole derivatives as potential antimicrobial agents
Yi-Jie Xue, Ming-Yue Li, Xue-Jun Jin, Chang-Ji Zheng & Hu-Ri Piao
Pages: 296-307
Published online: 06 Jan 2021
AbstractforDesign, synthesis and evaluation of carbazole derivatives as potential antimicrobial agents | Full Text | References | PDF (2.1 MB) | EPUB
  • 3628 Views
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Article
Novel piperazine–chalcone hybrids and related pyrazoline analogues targeting VEGFR-2 kinase; design, synthesis, molecular docking studies, and anticancer evaluation
Marwa F. Ahmed, Eman Y. Santali & Radwan El-Haggar
Pages: 308-319
Published online: 21 Dec 2020
AbstractforNovel piperazine–chalcone hybrids and related pyrazoline analogues targeting VEGFR-2 kinase; design, synthesis, molecular docking studies, and anticancer evaluation | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
  • 3637 Views
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Article
Development of 2-oxindolin-3-ylidene-indole-3-carbohydrazide derivatives as novel apoptotic and anti-proliferative agents towards colorectal cancer cells
Wagdy M. Eldehna, Mahmoud F. Abo-Ashour, Tarfah Al-Warhi, Sara T. Al-Rashood, Amal Alharbi, Rezk R. Ayyad, Khayal Al-Khayal, Maha Abdulla, Hatem A. Abdel-Aziz, Rehan Ahmad & Radwan El-Haggar
Pages: 320-329
Published online: 20 Dec 2020
AbstractforDevelopment of 2-oxindolin-3-ylidene-indole-3-carbohydrazide derivatives as novel apoptotic and anti-proliferative agents towards colorectal cancer cells | Full Text | References | PDF (1.8 MB) | EPUB | Supplemental
  • 2549 Views
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Brief Report
Inhibition of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with sulphonamides
Linda J. Urbański, Andrea Angeli, Vesa P. Hytönen, Anna Di Fiore, Giuseppina De Simone, Seppo Parkkila & Claudiu T. Supuran
Pages: 330-335
Published online: 28 Dec 2020
AbstractforInhibition of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with sulphonamides | Full Text | References | PDF (1.2 MB)
  • 1651 Views
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Article
Anticancer active trifluoromethylated fused triazinones are safe for early-life stages of zebrafish (Danio rerio) and reveal a proapoptotic action
Małgorzata Sztanke, Jolanta Rzymowska & Krzysztof Sztanke
Pages: 336-344
Published online: 04 Jan 2021
AbstractforAnticancer active trifluoromethylated fused triazinones are safe for early-life stages of zebrafish (Danio rerio) and reveal a proapoptotic action | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
  • 1604 Views
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Brief Report
Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety
Xu Han, Yun Long Yu, Duo Ma, Zhao Yan Zhang & Xin Hua Liu
Pages: 345-361
Published online: 27 Dec 2020
AbstractforSynthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
  • 2241 Views
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Thioredoxin-dependent system. Application of inhibitors
Anna Jastrząb & Elżbieta Skrzydlewska
Pages: 362-371
Published online: 27 Dec 2020
AbstractforThioredoxin-dependent system. Application of inhibitors | Full Text | References | PDF (1.4 MB) | EPUB
  • 3404 Views
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Article
Anion inhibition studies of the Zn(II)-bound ι-carbonic anhydrase from the Gram-negative bacterium Burkholderia territorii
Andrea Petreni, Viviana De Luca, Andrea Scaloni, Alessio Nocentini, Clemente Capasso & Claudiu T. Supuran
Pages: 372-376
Published online: 04 Jan 2021
AbstractforAnion inhibition studies of the Zn(II)-bound ι-carbonic anhydrase from the Gram-negative bacterium Burkholderia territorii | Full Text | References | PDF (888 KB)
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Brief Report
Pharmacophore-guided repurposing of fibrates and retinoids as GPR40 allosteric ligands with activity on insulin release
Erika Cione, Maria Cristina Caroleo, Hiroyuki Kagechika & Fabrizio Manetti
Pages: 377-383
Published online: 02 Feb 2021
AbstractforPharmacophore-guided repurposing of fibrates and retinoids as GPR40 allosteric ligands with activity on insulin release | Full Text | References | PDF (1.8 MB) | EPUB
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Article
Development of novel isatin–nicotinohydrazide hybrids with potent activity against susceptible/resistant Mycobacterium tuberculosis and bronchitis causing–bacteria
Zainab M. Elsayed, Wagdy M. Eldehna, Marwa M. Abdel-Aziz, Mahmoud A. El Hassab, Eslam B. Elkaeed, Tarfah Al-Warhi, Hatem A. Abdel-Aziz, Sahar M. Abou-Seri & Eman R. Mohammed
Pages: 384-392
Published online: 07 Jan 2021
AbstractforDevelopment of novel isatin–nicotinohydrazide hybrids with potent activity against susceptible/resistant Mycobacterium tuberculosis and bronchitis causing–bacteria | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
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Brief Report
Evaluating the efficiency of enzyme accelerated CO2 capture: chemical kinetics modelling for interpreting measurement results
Lorenzo Parri, Ada Fort, Anna Lo Grasso, Marco Mugnaini, Valerio Vignoli, Clemente Capasso, Sonia Del Prete, Maria Novella Romanelli & Claudiu T. Supuran
Pages: 393-400
Published online: 12 Jan 2021
AbstractforEvaluating the efficiency of enzyme accelerated CO2 capture: chemical kinetics modelling for interpreting measurement results | Full Text | References | PDF (3 MB) | EPUB
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Article
Development and characterisation of SMURF2-targeting modifiers
Dhanoop Manikoth Ayyathan, Gal Levy-Cohen, Moran Shubely, Sandy Boutros-Suleiman, Veronica Lepechkin-Zilbermintz, Michael Shokhen, Amnon Albeck, Arie Gruzman & Michael Blank
Pages: 401-409
Published online: 12 Jan 2021
AbstractforDevelopment and characterisation of SMURF2-targeting modifiers | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 2166 Views
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Article
Design, synthesis, and in vitro evaluation of BP-1-102 analogs with modified hydrophobic fragments for STAT3 inhibition
Patrik Oleksak, Miroslav Psotka, Marketa Vancurova, Olena Sapega, Jana Bieblova, Milan Reinis, David Rysanek, Romana Mikyskova, Katarina Chalupova, David Malinak, Jana Svobodova, Rudolf Andrys, Helena Rehulkova, Vojtech Skopek, Pham Ngoc Lam, Jiri Bartek, Zdenek Hodny & Kamil Musilek
Pages: 410-424
Published online: 13 Jan 2021
AbstractforDesign, synthesis, and in vitro evaluation of BP-1-102 analogs with modified hydrophobic fragments for STAT3 inhibition | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 2513 Views
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Article
Discovery of indole-3-butyric acid derivatives as potent histone deacetylase inhibitors
Yiming Chen, Lihui Zhang, Lin Zhang, Qixiao Jiang & Lei Zhang
Pages: 425-436
Published online: 14 Jan 2021
AbstractforDiscovery of indole-3-butyric acid derivatives as potent histone deacetylase inhibitors | Full Text | References | PDF (1.9 MB) | EPUB
  • 2809 Views
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Article
Pyridinium-2-carbaldoximes with quinolinium carboxamide moiety are simultaneous reactivators of acetylcholinesterase and butyrylcholinesterase inhibited by nerve agent surrogates
Hyun Myung Lee, Rudolf Andrys, Jakub Jonczyk, Kyuneun Kim, Avinash G. Vishakantegowda, David Malinak, Adam Skarka, Monika Schmidt, Michaela Vaskova, Kamil Latka, Marek Bajda, Young-Sik Jung, Barbara Malawska & Kamil Musilek
Pages: 437-449
Published online: 19 Jan 2021
AbstractforPyridinium-2-carbaldoximes with quinolinium carboxamide moiety are simultaneous reactivators of acetylcholinesterase and butyrylcholinesterase inhibited by nerve agent surrogates | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
  • 1643 Views
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Article
Synthesis and anti-rheumatoid arthritis activities of 3-(4-aminophenyl)-coumarin derivatives
Yuhang Miao, Jie Yang, Yinling Yun, Jie Sun & Xiaojing Wang
Pages: 450-461
Published online: 08 Feb 2021
AbstractforSynthesis and anti-rheumatoid arthritis activities of 3-(4-aminophenyl)-coumarin derivatives | Full Text | References | PDF (2.7 MB) | EPUB
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Brief Report
RETRACTED ARTICLE: Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors
Hyung Chul Ryu, Marc Windisch, Jee Woong Lim, Inhee Choi, Eun Kyu Lee, Hye Hyun Yoo & Tae Kon Kim
Pages: 462-468
Published online: 17 Jan 2021
AbstractforRETRACTED ARTICLE: Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors | Full Text | References | PDF (1.2 MB) | EPUB
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Article
Inhibition of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae with aromatic sulphonamides and clinically licenced drugs – a joint docking/molecular dynamics study
Alessandro Bonardi, Alessio Nocentini, Sameh Mohamed Osman, Fatmah Ali Alasmary, Tahani Mazyad Almutairi, Dalal Saied Abdullah, Paola Gratteri & Claudiu T. Supuran
Pages: 469-479
Published online: 20 Jan 2021
AbstractforInhibition of α-, β- and γ-carbonic anhydrases from the pathogenic bacterium Vibrio cholerae with aromatic sulphonamides and clinically licenced drugs – a joint docking/molecular dynamics study | Full Text | References | PDF (2.9 MB) | Supplemental
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Article
Structural insights and molecular dynamics into the inhibitory mechanism of a Kunitz-type trypsin inhibitor from Tamarindus indica L
Amanda Fernandes de Medeiros, Beatriz Blenda Pinheiro de Souza, Lucas Pinheiro Coutinho, Aline Melro Murad, Paula Ivani Medeiros dos Santos, Norberto de Kássio Vieira Monteiro, Elizeu Antunes dos Santos, Bruna Leal Lima Maciel & Ana Heloneida de Araújo Morais
Pages: 480-490
Published online: 24 Jan 2021
AbstractforStructural insights and molecular dynamics into the inhibitory mechanism of a Kunitz-type trypsin inhibitor from Tamarindus indica L | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
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Article
Discovery of new acetylcholinesterase inhibitors for Alzheimer’s disease: virtual screening and in vitro characterisation
Benoit David, Pascal Schneider, Philipp Schäfer, Jörg Pietruszka & Holger Gohlke
Pages: 491-496
Published online: 21 Jan 2021
AbstractforDiscovery of new acetylcholinesterase inhibitors for Alzheimer’s disease: virtual screening and in vitro characterisation | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
  • 5511 Views
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Article
Scutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro
Hongbo Liu, Fei Ye, Qi Sun, Hao Liang, Chunmei Li, Siyang Li, Roujian Lu, Baoying Huang, Wenjie Tan & Luhua Lai
Pages: 497-503
Published online: 24 Jan 2021
AbstractforScutellaria baicalensis extract and baicalein inhibit replication of SARS-CoV-2 and its 3C-like protease in vitro | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
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Article
Click chemistry based synthesis, cytotoxic activity and molecular docking of novel triazole-thienopyrimidine hybrid glycosides targeting EGFR
Reham R. Khattab, Asma K. Alshamari, Allam A. Hassan, Hussein H. Elganzory, Wael A. El-Sayed, Hanem M. Awad, Eman S. Nossier & Nasser A. Hassan
Pages: 504-516
Published online: 28 Jan 2021
AbstractforClick chemistry based synthesis, cytotoxic activity and molecular docking of novel triazole-thienopyrimidine hybrid glycosides targeting EGFR | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
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Article
Washingtonia filifera seed extracts inhibit the islet amyloid polypeptide fibrils formations and α-amylase and α-glucosidase activity
Sonia Floris, Antonella Fais, Rosaria Medda, Francesca Pintus, Alessandra Piras, Amit Kumar, Piotr Marek Kuś, Gunilla Torstensdotter Westermark & Benedetta Era
Pages: 517-524
Published online: 25 Jan 2021
AbstractforWashingtonia filifera seed extracts inhibit the islet amyloid polypeptide fibrils formations and α-amylase and α-glucosidase activity | Full Text | References | PDF (1.2 MB) | EPUB
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Article
Nitrous anhydrase activity of carbonic anhydrase II: cysteine is required for nitric oxide (NO) dependent phosphorylation of VASP in human platelets
Dimitrios Tsikas & Stepan Gambaryan
Pages: 525-534
Published online: 28 Jan 2021
AbstractforNitrous anhydrase activity of carbonic anhydrase II: cysteine is required for nitric oxide (NO) dependent phosphorylation of VASP in human platelets | Full Text | References | PDF (1.4 MB) | EPUB
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Article
Exploration of novel heterofused 1,2,4-triazine derivative in colorectal cancer
Justyna Magdalena Hermanowicz, Anna Szymanowska, Beata Sieklucka, Robert Czarnomysy, Krystyna Pawlak, Anna Bielawska, Krzysztof Bielawski, Joanna Kalafut, Alicja Przybyszewska, Arkadiusz Surazynski, Adolfo Rivero-Muller, Mariusz Mojzych & Dariusz Pawlak
Pages: 535-548
Published online: 31 Jan 2021
AbstractforExploration of novel heterofused 1,2,4-triazine derivative in colorectal cancer | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
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Article
Design, synthesis and biological evaluation of 1-Aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as novel microtubule destabilizers
Chao Wang, Yuelin Li, Zi Liu, Zeyu Wang, Zihan Liu, Shuai Man, Yujing Zhang, Kai Bao, Yingliang Wu, Qi Guan, Daiying Zuo & Weige Zhang
Pages: 549-560
Published online: 31 Jan 2021
AbstractforDesign, synthesis and biological evaluation of 1-Aryl-5-(4-arylpiperazine-1-carbonyl)-1H-tetrazols as novel microtubule destabilizers | Full Text | References | PDF (2 MB) | EPUB
  • 1931 Views
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Reconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase
Alessio Nocentini, Andrea Angeli, Fabrizio Carta, Jean-Yves Winum, Raivis Zalubovskis, Simone Carradori, Clemente Capasso, William A. Donald & Claudiu T. Supuran
Pages: 561-580
Published online: 21 Feb 2021
AbstractforReconsidering anion inhibitors in the general context of drug design studies of modulators of activity of the classical enzyme carbonic anhydrase | Full Text | References | PDF (3.2 MB)
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Article
Reliable chromatographic assay for measuring of indoleamine 2,3-dioxygenase 1 (IDO1) activity in human cancer cells
Ilona Sadok, Kamila Rachwał, Ilona Jonik & Magdalena Staniszewska
Pages: 581-592
Published online: 04 Feb 2021
AbstractforReliable chromatographic assay for measuring of indoleamine 2,3-dioxygenase 1 (IDO1) activity in human cancer cells | Full Text | References | PDF (2 MB) | EPUB
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Article
Design, synthesis, and evaluation of novel coumarin-dithiocarbamate derivatives (IDs) as anti-colorectal cancer agents
Heping Zhu, Shilong Ying, Bingluo Zhou, Xinyang Hu, Xiao Liang, Wangyu Li, Dungai Wang, Hongchuan Jin & Yuanjiang Pan
Pages: 593-604
Published online: 08 Feb 2021
AbstractforDesign, synthesis, and evaluation of novel coumarin-dithiocarbamate derivatives (IDs) as anti-colorectal cancer agents | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Article
Solubility enhancement of mefenamic acid by inclusion complex with β-cyclodextrin: in silico modelling, formulation, characterisation, and in vitro studies
Dounia Sid, Milad Baitiche, Zineb Elbahri, Ferhat Djerboua, Mokhtar Boutahala, Zouhair Bouaziz & Marc Le Borgne
Pages: 605-617
Published online: 08 Feb 2021
AbstractforSolubility enhancement of mefenamic acid by inclusion complex with β-cyclodextrin: in silico modelling, formulation, characterisation, and in vitro studies | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
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Article
Phytochemical profile, enzyme inhibition activity and molecular docking analysis of Feijoa sellowiana O. Berg
Fatema R. Saber, Rehab M. Ashour, Ali M. El-Halawany, Mohamad Fawzi Mahomoodally, Gunes Ak, Gokhan Zengin & Engy A. Mahrous
Pages: 618-626
Published online: 08 Feb 2021
AbstractforPhytochemical profile, enzyme inhibition activity and molecular docking analysis of Feijoa sellowiana O. Berg | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
  • 3391 Views
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Article
New 3-O-substituted xanthone derivatives as promising acetylcholinesterase inhibitors
Zi Han Loh, Huey Chong Kwong, Kok Wai Lam, Soek Sin Teh, Gwendoline Cheng Lian Ee, Ching Kheng Quah, Anthony Siong Hock Ho & Siau Hui Mah
Pages: 627-639
Published online: 08 Feb 2021
AbstractforNew 3-O-substituted xanthone derivatives as promising acetylcholinesterase inhibitors | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
  • 2287 Views
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Article
Discovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation
Mohamed Hagras, Moshira A. El Deeb, Heba S. A. Elzahabi, Eslam B. Elkaeed, Ahmed B. M. Mehany & Ibrahim H. Eissa
Pages: 640-658
Published online: 15 Feb 2021
AbstractforDiscovery of new quinolines as potent colchicine binding site inhibitors: design, synthesis, docking studies, and anti-proliferative evaluation | Full Text | References | PDF (4 MB) | EPUB | Supplemental
  • 2960 Views
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Article
Exposure of human intestinal epithelial cells and primary human hepatocytes to trypsin-like serine protease inhibitors with potential antiviral effect
Erzsébet Pászti-Gere, Judit Pomothy, Ákos Jerzsele, Oliver Pilgram & Torsten Steinmetzer
Pages: 659-668
Published online: 01 Mar 2021
AbstractforExposure of human intestinal epithelial cells and primary human hepatocytes to trypsin-like serine protease inhibitors with potential antiviral effect | Full Text | References | PDF (2.1 MB) | EPUB
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Article
Challenging inflammatory process at molecular, cellular and in vivo levels via some new pyrazolyl thiazolones
Perihan A. Elzahhar, Rana A. Alaaeddine, Rasha Nassra, Azza Ismail, Hala F. Labib, Mohamed G. Temraz, Ahmed S. F. Belal & Ahmed F. El-Yazbi
Pages: 669-684
Published online: 22 Feb 2021
AbstractforChallenging inflammatory process at molecular, cellular and in vivo levels via some new pyrazolyl thiazolones | Full Text | References | PDF (3.8 MB) | EPUB | Supplemental
  • 2013 Views
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Brief Report
Selective inhibition of carbonic anhydrase IX and XII by coumarin and psoralen derivatives
Rita Meleddu, Serenella Deplano, Elias Maccioni, Francesco Ortuso, Filippo Cottiglia, Daniela Secci, Alessia Onali, Erica Sanna, Andrea Angeli, Rossella Angius, Stefano Alcaro, Claudiu T. Supuran & Simona Distinto
Pages: 685-692
Published online: 18 Feb 2021
AbstractforSelective inhibition of carbonic anhydrase IX and XII by coumarin and psoralen derivatives | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
  • 1969 Views
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Small molecule inhibitors of cyclin-dependent kinase 9 for cancer therapy
Aisha Alsfouk
Pages: 693-706
Published online: 25 Feb 2021
AbstractforSmall molecule inhibitors of cyclin-dependent kinase 9 for cancer therapy | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 3861 Views
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Article
Discovery of potent histone deacetylase inhibitors with modified phenanthridine caps
Wenli Fan, Lin Zhang, Xuejiang Wang, Haiyong Jia & Lei Zhang
Pages: 707-718
Published online: 05 Mar 2021
AbstractforDiscovery of potent histone deacetylase inhibitors with modified phenanthridine caps | Full Text | References | PDF (3.4 MB) | EPUB
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Article
Activation of carbonic anhydrase isoforms involved in modulation of emotional memory and cognitive disorders with histamine agonists, antagonists and derivatives
Gustavo Provensi, Alessio Nocentini, Maria Beatrice Passani, Patrizio Blandina & Claudiu T. Supuran
Pages: 719-726
Published online: 02 Mar 2021
AbstractforActivation of carbonic anhydrase isoforms involved in modulation of emotional memory and cognitive disorders with histamine agonists, antagonists and derivatives | Full Text | References | PDF (1.1 MB)
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Article
In silico identification of novel SARS-COV-2 2′-O-methyltransferase (nsp16) inhibitors: structure-based virtual screening, molecular dynamics simulation and MM-PBSA approaches
Mahmoud A. El Hassab, Tamer M. Ibrahim, Sara T. Al-Rashood, Amal Alharbi, Razan O. Eskandrani & Wagdy M. Eldehna
Pages: 727-736
Published online: 09 Mar 2021
AbstractforIn silico identification of novel SARS-COV-2 2′-O-methyltransferase (nsp16) inhibitors: structure-based virtual screening, molecular dynamics simulation and MM-PBSA approaches | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Article
The development of novel cytochrome P450 2J2 (CYP2J2) inhibitor and the underlying interaction between inhibitor and CYP2J2
Xiangge Tian, Meirong Zhou, Jing Ning, Xiaopeng Deng, Lei Feng, Huilian Huang, Dahong Yao & Xiaochi Ma
Pages: 737-748
Published online: 07 Mar 2021
AbstractforThe development of novel cytochrome P450 2J2 (CYP2J2) inhibitor and the underlying interaction between inhibitor and CYP2J2 | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
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Article
Flavonoids and Acid-Hydrolysis derivatives of Neo-Clerodane diterpenes from Teucrium flavum subsp. glaucum as inhibitors of the HIV-1 reverse transcriptase–associated RNase H function
Benedetta Fois, Angela Corona, Enzo Tramontano, Simona Distinto, Elias Maccioni, Rita Meleddu, Pierluigi Caboni, Costantino Floris & Filippo Cottiglia
Pages: 749-757
Published online: 10 Mar 2021
AbstractforFlavonoids and Acid-Hydrolysis derivatives of Neo-Clerodane diterpenes from Teucrium flavum subsp. glaucum as inhibitors of the HIV-1 reverse transcriptase–associated RNase H function | Full Text | References | PDF (1.9 MB) | Supplemental
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Brief Report
Activation of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with amines and amino acids
Andrea Angeli, Linda J. Urbański, Vesa P. Hytönen, Seppo Parkkila & Claudiu T. Supuran
Pages: 758-763
Published online: 10 Mar 2021
AbstractforActivation of the β-carbonic anhydrase from the protozoan pathogen Trichomonas vaginalis with amines and amino acids | Full Text | References | PDF (1.1 MB)
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Article
Synthesis, biological activities and docking studies of pleuromutilin derivatives with piperazinyl urea linkage
Yuanyuan Zhang, Chuan Xie, Yang Liu, Feng Shang, Rushiya Shao, Jing Yu, Chunxia Wu, Xinghui Yao, Dongfang Liu & Zhouyu Wang
Pages: 764-775
Published online: 18 Mar 2021
AbstractforSynthesis, biological activities and docking studies of pleuromutilin derivatives with piperazinyl urea linkage | Full Text | References | PDF (2.2 MB) | EPUB
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Article
A study of inhibitors of d-glycero-β-d-manno-heptose-1-phosphate adenylyltransferase from Burkholderia pseudomallei as a potential antibiotic target
Suwon Kim, Seri Jo, Mi-Sun Kim & Dong Hae Shin
Pages: 776-784
Published online: 18 Mar 2021
AbstractforA study of inhibitors of d-glycero-β-d-manno-heptose-1-phosphate adenylyltransferase from Burkholderia pseudomallei as a potential antibiotic target | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
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Article
Platelet hyaluronidase 2 enrichment in acute coronary syndromes: a conceivable role in monocyte-platelet aggregate formation
Ramona Vinci, Daniela Pedicino, Alessia D’Aiello, Pellegrino Ciampi, Myriana Ponzo, Alice Bonanni, Giulio Russo, Rocco Antonio Montone, Massimo Massetti, Filippo Crea & Giovanna Liuzzo
Pages: 785-789
Published online: 18 Mar 2021
AbstractforPlatelet hyaluronidase 2 enrichment in acute coronary syndromes: a conceivable role in monocyte-platelet aggregate formation | Full Text | References | PDF (1 MB) | EPUB
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Article
Onopordopicrin from the new genus Shangwua as a novel thioredoxin reductase inhibitor to induce oxidative stress-mediated tumor cell apoptosis
Junmin Zhang, Zai-Qin Zheng, Qianhe Xu, Ya Li, Kun Gao & Jianguo Fang
Pages: 790-801
Published online: 18 Mar 2021
AbstractforOnopordopicrin from the new genus Shangwua as a novel thioredoxin reductase inhibitor to induce oxidative stress-mediated tumor cell apoptosis | Full Text | References | PDF (3 MB) | EPUB
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Article
Discovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect
Tarek S. Ibrahim, Mohamed M. Hawwas, Azizah M. Malebari, Ehab S. Taher, Abdelsattar M. Omar, Thikryat Neamatallah, Zakaria K. Abdel-Samii, Martin K. Safo & Yaseen A. M. M. Elshaier
Pages: 802-818
Published online: 18 Mar 2021
AbstractforDiscovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect | Full Text | References | PDF (3.6 MB) | EPUB
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Article
Inhibition of bacterial and human zinc-metalloproteases by bisphosphonate- and catechol-containing compounds
Fatema Rahman, Tra-Mi Nguyen, Olayiwola A. Adekoya, Cristina Campestre, Paolo Tortorella, Ingebrigt Sylte & Jan-Olof Winberg
Pages: 819-830
Published online: 23 Mar 2021
AbstractforInhibition of bacterial and human zinc-metalloproteases by bisphosphonate- and catechol-containing compounds | Full Text | References | PDF (2.7 MB) | EPUB
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Article
The translocator protein ligands as mitochondrial functional modulators for the potential anti-Alzheimer agents
TaeHun Kim, Mohammad N. Morshed, Ashwini M. Londhe, Ji W. Lim, Ha E. Lee, Suengmok Cho, Sung J. Cho, Hayoung Hwang, Sang M. Lim, Jae Y. Lee, Jiyoun Lee & Ae N. Pae
Pages: 831-846
Published online: 23 Mar 2021
AbstractforThe translocator protein ligands as mitochondrial functional modulators for the potential anti-Alzheimer agents | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
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Article
8-Mercaptoguanine-based inhibitors of Mycobacterium tuberculosis dihydroneopterin aldolase: synthesis, in vitro inhibition and docking studies
Alexia de Matos Czeczot, Candida Deves Roth, Rodrigo Gay Ducati, Kenia Pissinate, Raoní Scheibler Rambo, Luís Fernando Saraiva Macedo Timmers, Bruno Lopes Abbadi, Fernanda Souza Macchi, Víctor Zajaczkowski Pestana, Luiz Augusto Basso, Pablo Machado & Cristiano Valim Bizarro
Pages: 847-855
Published online: 23 Mar 2021
Abstractfor8-Mercaptoguanine-based inhibitors of Mycobacterium tuberculosis dihydroneopterin aldolase: synthesis, in vitro inhibition and docking studies | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Article
Modulation of SETDB1 activity by APQ ameliorates heterochromatin condensation, motor function, and neuropathology in a Huntington’s disease mouse model
Yu Jin Hwang, Seung Jae Hyeon, Younghee Kim, Sungsu Lim, Min Young Lee, Jieun Kim, Ashwini M. Londhe, Lizaveta Gotina, Yunha Kim, Ae Nim Pae, Yong Seo Cho, Jihye Seong, Hyemyung Seo, Yun Kyung Kim, Hyunah Choo, Hoon Ryu & Sun-Joon Min
Pages: 856-868
Published online: 26 Mar 2021
AbstractforModulation of SETDB1 activity by APQ ameliorates heterochromatin condensation, motor function, and neuropathology in a Huntington’s disease mouse model | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
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Article
In vitro anti-TB properties, in silico target validation, molecular docking and dynamics studies of substituted 1,2,4-oxadiazole analogues against Mycobacterium tuberculosis
Pran Kishore Deb, Nizar A. Al-Shar’i, Katharigatta N. Venugopala, Melendhran Pillay & Pobitra Borah
Pages: 869-884
Published online: 01 Jun 2021
AbstractforIn vitro anti-TB properties, in silico target validation, molecular docking and dynamics studies of substituted 1,2,4-oxadiazole analogues against Mycobacterium tuberculosis | Full Text | References | PDF (4.4 MB) | EPUB
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Article
Dietary inclusion of royal jelly modulates gene expression and activity of oxidative stress enzymes in zebrafish
Ercüment Aksakal, Deniz Ekinci & Claudiu T. Supuran
Pages: 885-894
Published online: 23 Mar 2021
AbstractforDietary inclusion of royal jelly modulates gene expression and activity of oxidative stress enzymes in zebrafish | Full Text | References | PDF (2.1 MB) | EPUB
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Article
Transition metal-catalysed A-ring C–H activations and C(sp2)–C(sp2) couplings in the 13α-oestrone series and in vitro evaluation of antiproliferative properties
Péter Traj, Ali Hazhmat Abdolkhaliq, Anett Németh, Sámuel Trisztán Dajcs, Ferenc Tömösi, Tea Lanisnik-Rizner, István Zupkó & Erzsébet Mernyák
Pages: 895-902
Published online: 26 Mar 2021
AbstractforTransition metal-catalysed A-ring C–H activations and C(sp2)–C(sp2) couplings in the 13α-oestrone series and in vitro evaluation of antiproliferative properties | Full Text | References | PDF (871.9 KB) | EPUB | Supplemental
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Article
Discovery of the natural product 3',4',7,8-tetrahydroxyflavone as a novel and potent selective BRD4 bromodomain 2 inhibitor
Jiao Li, Wei Zou, Koukou Yu, Bing Liu, Weifeng Liang, Lisha Wang, Yin Lu, Zequn Jiang, Aiyun Wang & Jiapeng Zhu
Pages: 903-913
Published online: 06 Apr 2021
AbstractforDiscovery of the natural product 3',4',7,8-tetrahydroxyflavone as a novel and potent selective BRD4 bromodomain 2 inhibitor | Full Text | References | PDF (3.2 MB) | EPUB
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Article
Structural determinants for subnanomolar inhibition of the secreted aspartic protease Sapp1p from Candida parapsilosis
Jiří Dostál, Jiří Brynda, Lucie Vaňková, Syeda Rehana Zia, Iva Pichová, Olga Heidingsfeld & Martin Lepšík
Pages: 914-921
Published online: 11 Apr 2021
AbstractforStructural determinants for subnanomolar inhibition of the secreted aspartic protease Sapp1p from Candida parapsilosis | Full Text | References | PDF (1.8 MB) | EPUB
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Article
Design, synthesis, anticancer evaluation, and molecular modelling studies of novel tolmetin derivatives as potential VEGFR-2 inhibitors and apoptosis inducers
Asmaa E. Kassab, Ehab M. Gedawy, Mohammed I. A. Hamed, Ahmed S. Doghish & Rasha A. Hassan
Pages: 922-939
Published online: 26 Apr 2021
AbstractforDesign, synthesis, anticancer evaluation, and molecular modelling studies of novel tolmetin derivatives as potential VEGFR-2 inhibitors and apoptosis inducers | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
  • 2693 Views
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Article
Design, synthesis and in vitro and in vivo biological evaluation of flurbiprofen amides as new fatty acid amide hydrolase/cyclooxygenase-2 dual inhibitory potential analgesic agents
Alessandro Deplano, Jessica Karlsson, Federica Moraca, Mona Svensson, Claudia Cristiano, Carmine Marco Morgillo, Christopher J. Fowler, Roberto Russo, Bruno Catalanotti & Valentina Onnis
Pages: 940-953
Published online: 26 Apr 2021
AbstractforDesign, synthesis and in vitro and in vivo biological evaluation of flurbiprofen amides as new fatty acid amide hydrolase/cyclooxygenase-2 dual inhibitory potential analgesic agents | Full Text | References | PDF (3.4 MB) | EPUB | Supplemental
  • 1972 Views
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Article
Anti-breast cancer action of carbonic anhydrase IX inhibitor 4-[4-(4-Benzo[1,3]dioxol-5-ylmethyl-piperazin-1-yl)-benzylidene-hydrazinocarbonyl]-benzenesulfonamide (BSM-0004): in vitro and in vivo studies
Chandra Bhushan Mishra, Raj Kumar Mongre, Amresh Prakash, Raok Jeon, Claudiu T. Supuran & Myeong-Sok Lee
Pages: 954-963
Published online: 05 May 2021
AbstractforAnti-breast cancer action of carbonic anhydrase IX inhibitor 4-[4-(4-Benzo[1,3]dioxol-5-ylmethyl-piperazin-1-yl)-benzylidene-hydrazinocarbonyl]-benzenesulfonamide (BSM-0004): in vitro and in vivo studies | Full Text | References | PDF (2.7 MB) | EPUB
  • 1782 Views
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Brief Report
Protective effects of carbonic anhydrase inhibition in brain ischaemia in vitro and in vivo models
Ilaria Dettori, Irene Fusco, Irene Bulli, Lisa Gaviano, Elisabetta Coppi, Federica Cherchi, Martina Venturini, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Alessio Nocentini, Claudiu T. Supuran, Anna Maria Pugliese & Felicita Pedata
Pages: 964-976
Published online: 31 May 2021
AbstractforProtective effects of carbonic anhydrase inhibition in brain ischaemia in vitro and in vivo models | Full Text | References | PDF (3.6 MB) | EPUB
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Article
Utility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition
Rania H. Abd El-Hameed, Shahenda Mahgoub, Hend M. El-Shanbaky, Mosaad S. Mohamed & Sahar A. Ali
Pages: 977-986
Published online: 06 May 2021
AbstractforUtility of novel 2-furanones in synthesis of other heterocyclic compounds having anti-inflammatory activity with dual COX2/LOX inhibition | Full Text | References | PDF (1 MB) | EPUB | Supplemental
  • 1909 Views
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Article
Development of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells
Mohammad M. Al-Sanea, Ghada H. Al-Ansary, Zainab M. Elsayed, Raed M. Maklad, Eslam B. Elkaeed, Mohamed A. Abdelgawad, Syed Nasir Abbas Bukhari, Marwa M. Abdel-Aziz, Howayda Suliman & Wagdy M. Eldehna
Pages: 987-999
Published online: 13 May 2021
AbstractforDevelopment of 3-methyl/3-(morpholinomethyl)benzofuran derivatives as novel antitumor agents towards non-small cell lung cancer cells | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
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Article
Effect of amino acids and amines on the activity of the recombinant ι-carbonic anhydrase from the Gram-negative bacterium Burkholderia territorii
Viviana De Luca, Andrea Petreni, Vincenzo Carginale, Andrea Scaloni, Claudiu T. Supuran & Clemente Capasso
Pages: 1000-1006
Published online: 13 May 2021
AbstractforEffect of amino acids and amines on the activity of the recombinant ι-carbonic anhydrase from the Gram-negative bacterium Burkholderia territorii | Full Text | References | PDF (1 MB) | EPUB
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Brief Report
Identification of a novel SPT inhibitor WXP-003 by docking-based virtual screening and investigation of its anti-fungi effect
Xin Wang, Xin Yang, Xin Sun, Yi Qian, Mengyao Fan, Zhehao Zhang, Kaiyuan Deng, Zaixiang Lou, Zejun Pei & Jingyu Zhu
Pages: 1007-1015
Published online: 21 Jun 2021
AbstractforIdentification of a novel SPT inhibitor WXP-003 by docking-based virtual screening and investigation of its anti-fungi effect | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Flavonoids as inhibitors of human neutrophil elastase
Katarzyna Jakimiuk, Jakub Gesek, Atanas G. Atanasov & Michał Tomczyk
Pages: 1016-1028
Published online: 13 May 2021
AbstractforFlavonoids as inhibitors of human neutrophil elastase | Full Text | References | PDF (1.8 MB) | EPUB
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Article
Methoxy and bromo scans on N-(5-methoxyphenyl) methoxybenzenesulphonamides reveal potent cytotoxic compounds, especially against the human breast adenocarcinoma MCF7 cell line
Myriam González, María Ovejero-Sánchez, Alba Vicente-Blázquez, Manuel Medarde, Rogelio González-Sarmiento & Rafael Peláez
Pages: 1029-1047
Published online: 09 Jun 2021
AbstractforMethoxy and bromo scans on N-(5-methoxyphenyl) methoxybenzenesulphonamides reveal potent cytotoxic compounds, especially against the human breast adenocarcinoma MCF7 cell line | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
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Retraction
Statement of retraction: [thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors]
Page: 1048
Published online: 24 Jun 2021
CitationforStatement of retraction: [thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors] | Full Text | PDF (19.6 KB) | EPUB
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Article
Inhibition of soluble epoxide hydrolase by phytochemical constituents of the root bark of Ulmus davidiana var. japonica
Jang Hoon Kim, Ji Su Park, Yun Ji Lee, Sena Choi, Young Ho Kim & Seo Young Yang
Pages: 1049-1055
Published online: 17 May 2021
AbstractforInhibition of soluble epoxide hydrolase by phytochemical constituents of the root bark of Ulmus davidiana var. japonica | Full Text | References | PDF (1.6 MB) | EPUB | Supplemental
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Article
Biochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida®) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms
Claudiu T. Supuran, Alessio Nocentini, Elena Yakubova, Nikolay Savchuk, Stanislav Kalinin & Mikhail Krasavin
Pages: 1056-1060
Published online: 17 May 2021
AbstractforBiochemical profiling of anti-HIV prodrug Elsulfavirine (Elpida®) and its active form VM1500A against a panel of twelve human carbonic anhydrase isoforms | Full Text | References | PDF (1.1 MB)
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Article
Anion inhibition studies of the α-carbonic anhydrases from Neisseria gonorrhoeae
Alessio Nocentini, Chad S. Hewitt, Margaret D. Mastrolorenzo, Daniel P. Flaherty & Claudiu T. Supuran
Pages: 1061-1066
Published online: 24 May 2021
AbstractforAnion inhibition studies of the α-carbonic anhydrases from Neisseria gonorrhoeae | Full Text | References | PDF (1.1 MB)
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Article
Novel chalcone/aryl carboximidamide hybrids as potent anti-inflammatory via inhibition of prostaglandin E2 and inducible NO synthase activities: design, synthesis, molecular docking studies and ADMET prediction
Tarek S. Ibrahim, Amr H. Moustafa, Ahmad J. Almalki, Rasha M. Allam, Abdulhamid Althagafi, Shadab Md & Mamdouh F. A. Mohamed
Pages: 1067-1078
Published online: 24 May 2021
AbstractforNovel chalcone/aryl carboximidamide hybrids as potent anti-inflammatory via inhibition of prostaglandin E2 and inducible NO synthase activities: design, synthesis, molecular docking studies and ADMET prediction | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Article
Inhibition of catechol-O-methyltransferase by natural pentacyclic triterpenes: structure–activity relationships and kinetic mechanism
Fang-Yuan Wang, Gui-Lin Wei, Yu-Fan Fan, Dong-Fang Zhao, Ping Wang, Li-Wei Zou & Ling Yang
Pages: 1079-1087
Published online: 24 May 2021
AbstractforInhibition of catechol-O-methyltransferase by natural pentacyclic triterpenes: structure–activity relationships and kinetic mechanism | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Brief Report
An anion and small molecule inhibition study of the β-carbonic anhydrase from Staphylococcus aureus
Linda J. Urbanski, Daniela Vullo, Seppo Parkkila & Claudiu T. Supuran
Pages: 1088-1092
Published online: 31 May 2021
AbstractforAn anion and small molecule inhibition study of the β-carbonic anhydrase from Staphylococcus aureus | Full Text | References | PDF (782.1 KB)
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Article
Discovery of new VEGFR-2 inhibitors based on bis([1, 2, 4]triazolo)[4,3-a:3',4'-c]quinoxaline derivatives as anticancer agents and apoptosis inducers
Nawaf A. Alsaif, Mohammed S. Taghour, Mohammed M. Alanazi, Ahmad J. Obaidullah, Abdulrahman A. Al-Mehizia, Manal M. Alanazi, Saleh Aldawas, Alaa Elwan & Hazem Elkady
Pages: 1093-1114
Published online: 31 May 2021
AbstractforDiscovery of new VEGFR-2 inhibitors based on bis([1, 2, 4]triazolo)[4,3-a:3',4'-c]quinoxaline derivatives as anticancer agents and apoptosis inducers | Full Text | References | PDF (5.1 MB) | EPUB | Supplemental
  • 2153 Views
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Application of triazoles in the structural modification of natural products
Hong-Yan Guo, Zheng-Ai Chen, Qing-Kun Shen & Zhe-Shan Quan
Pages: 1115-1144
Published online: 24 Jun 2021
AbstractforApplication of triazoles in the structural modification of natural products | Full Text | References | PDF (3.4 MB) | EPUB
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Article
4-Arylthiosemicarbazide derivatives as a new class of tyrosinase inhibitors and anti-Toxoplasma gondii agents
Adrian Bekier, Lidia Węglińska, Agata Paneth, Piotr Paneth & Katarzyna Dzitko
Pages: 1145-1164
Published online: 02 Jun 2021
Abstractfor4-Arylthiosemicarbazide derivatives as a new class of tyrosinase inhibitors and anti-Toxoplasma gondii agents | Full Text | References | PDF (6 MB) | EPUB | Supplemental
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Piperazine skeleton in the structural modification of natural products: a review
Run-Hui Zhang, Hong-Yan Guo, Hao Deng, Jinzi Li & Zhe-Shan Quan
Pages: 1165-1197
Published online: 03 Jun 2021
AbstractforPiperazine skeleton in the structural modification of natural products: a review | Full Text | References | PDF (5.9 MB) | EPUB
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Article
Structure-based virtual screening of highly potent inhibitors of the nematode chitinase CeCht1
Wei Chen, Qi Chen, Ashutosh Kumar, Xi Jiang, Kam Y. J. Zhang & Qing Yang
Pages: 1198-1204
Published online: 02 Jun 2021
AbstractforStructure-based virtual screening of highly potent inhibitors of the nematode chitinase CeCht1 | Full Text | References | PDF (2.6 MB) | EPUB
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Brief Report
Synthesis and preliminary structure-activity relationship study of 3-methylquinazolinone derivatives as EGFR inhibitors with enhanced antiproliferative activities against tumour cells
Yan Zhang, Qin Wang, Luolan Li, Yi Le, Li Liu, Jing Yang, Yongliang Li, Guochen Bao & Longjia Yan
Pages: 1205-1216
Published online: 02 Jun 2021
AbstractforSynthesis and preliminary structure-activity relationship study of 3-methylquinazolinone derivatives as EGFR inhibitors with enhanced antiproliferative activities against tumour cells | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
  • 1954 Views
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Article
Synthesis and biological evaluation of thiazolidinedione derivatives with high ligand efficiency to P. aeruginosa PhzS
Thamires Quadros Froes, Bianca Trindade Chaves, Marina Sena Mendes, Rafael Matos Ximenes, Ivanildo Mangueira da Silva, Priscila Brandão Gomes da Silva, Julianna Ferreira Cavalcanti de Albuquerque & Marcelo Santos Castilho
Pages: 1217-1229
Published online: 03 Jun 2021
AbstractforSynthesis and biological evaluation of thiazolidinedione derivatives with high ligand efficiency to P. aeruginosa PhzS | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
  • 1955 Views
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Brief Report
Is carbonic anhydrase inhibition useful as a complementary therapy of Covid-19 infection?
Secil Deniz, Tugba Kevser Uysal, Clemente Capasso, Claudiu T. Supuran & Ozen Ozensoy Guler
Pages: 1230-1235
Published online: 02 Jun 2021
AbstractforIs carbonic anhydrase inhibition useful as a complementary therapy of Covid-19 infection? | Full Text | References | PDF (1.2 MB) | EPUB
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Article
Synthesis and biological evaluation of 4-phenoxy-phenyl isoxazoles as novel acetyl-CoA carboxylase inhibitors
Xin Wu, Yongbo Yu & Tonghui Huang
Pages: 1236-1247
Published online: 08 Jun 2021
AbstractforSynthesis and biological evaluation of 4-phenoxy-phenyl isoxazoles as novel acetyl-CoA carboxylase inhibitors | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
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Article
Phenyl-substituted aminomethylene-bisphosphonates inhibit human P5C reductase and show antiproliferative activity against proline-hyperproducing tumour cells
Giuseppe Forlani, Giuseppe Sabbioni, Daniele Ragno, Davide Petrollino & Monica Borgatti
Pages: 1248-1257
Published online: 09 Jun 2021
AbstractforPhenyl-substituted aminomethylene-bisphosphonates inhibit human P5C reductase and show antiproliferative activity against proline-hyperproducing tumour cells | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Of mitochondrion and COVID-19
Khalid Omer Alfarouk, Sari T. S. Alhoufie, Abdelhameed Hifny, Laurent Schwartz, Ali S. Alqahtani, Samrein B. M. Ahmed, Ali M. Alqahtani, Saad S. Alqahtani, Abdel Khalig Muddathir, Heyam Ali, Adil H. H. Bashir, Muntaser E. Ibrahim, Maria Raffaella Greco, Rosa A. Cardone, Salvador Harguindey & Stephan Joel Reshkin
Pages: 1258-1266
Published online: 09 Jun 2021
AbstractforOf mitochondrion and COVID-19 | Full Text | References | PDF (1.1 MB) | EPUB
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Article
Latency, thermal stability, and identification of an inhibitory compound of mirolysin, a secretory protease of the human periodontopathogen Tannerella forsythia
Krzysztof M. Zak, Mark J. Bostock, Irena Waligorska, Ida B. Thøgersen, Jan J. Enghild, Grzegorz M. Popowicz, Przemyslaw Grudnik, Jan Potempa & Miroslaw Ksiazek
Pages: 1267-1281
Published online: 01 Jul 2021
AbstractforLatency, thermal stability, and identification of an inhibitory compound of mirolysin, a secretory protease of the human periodontopathogen Tannerella forsythia | Full Text | References | PDF (3 MB) | EPUB | Supplemental
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Article
Inhibiting PHGDH with NCT-503 reroutes glucose-derived carbons into the TCA cycle, independently of its on-target effect
Birte Arlt, Guido Mastrobuoni, Jasmin Wuenschel, Kathy Astrahantseff, Angelika Eggert, Stefan Kempa & Hedwig E. Deubzer
Pages: 1282-1289
Published online: 30 Jun 2021
AbstractforInhibiting PHGDH with NCT-503 reroutes glucose-derived carbons into the TCA cycle, independently of its on-target effect | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Article
Molecular design, synthesis and in vitro biological evaluation of thienopyrimidine–hydroxamic acids as chimeric kinase HDAC inhibitors: a challenging approach to combat cancer
Mona M. Abdel-Atty, Nahla A. Farag, Rabah A. T. Serya, Khaled A. M. Abouzid & Samar Mowafy
Pages: 1290-1311
Published online: 30 Jun 2021
AbstractforMolecular design, synthesis and in vitro biological evaluation of thienopyrimidine–hydroxamic acids as chimeric kinase HDAC inhibitors: a challenging approach to combat cancer | Full Text | References | PDF (4.1 MB) | EPUB | Supplemental
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Article
Novel pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety: design, synthesis, molecular docking, and biological evaluation as potential multi-target cytotoxic agents
Ahmed M. Shawky, Nashwa A. Ibrahim, Ashraf N. Abdalla, Mohammed A. S. Abourehab & Ahmed M. Gouda
Pages: 1312-1332
Published online: 21 Jun 2021
AbstractforNovel pyrrolizines bearing 3,4,5-trimethoxyphenyl moiety: design, synthesis, molecular docking, and biological evaluation as potential multi-target cytotoxic agents | Full Text | References | PDF (5.2 MB) | EPUB | Supplemental
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Article
Targeting allosteric sites of human aromatase: a comprehensive in-silico and in-vitro workflow to find potential plant-based anti-breast cancer therapeutics
Hani A. Alhadrami, Ahmed M. Sayed, Sami A. Melebari, Asem A. Khogeer, Wesam H. Abdulaal, Mohamed B. Al-Fageeh, Mohammad Algahtani & Mostafa E. Rateb
Pages: 1333-1344
Published online: 17 Jun 2021
AbstractforTargeting allosteric sites of human aromatase: a comprehensive in-silico and in-vitro workflow to find potential plant-based anti-breast cancer therapeutics | Full Text | References | PDF (4.1 MB) | EPUB | Supplemental
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Synthesis and biological evaluation of 2-arylbenzofuran derivatives as potential anti-Alzheimer’s disease agents
Yinling Yun, Yuhang Miao, Xiaoya Sun, Jie Sun & Xiaojing Wang
Pages: 1345-1355
Published online: 16 Jun 2021
AbstractforSynthesis and biological evaluation of 2-arylbenzofuran derivatives as potential anti-Alzheimer’s disease agents | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Tetralone derivatives are MIF tautomerase inhibitors and attenuate macrophage activation and amplify the hypothermic response in endotoxemic mice
János Garai, Marcell Krekó, László Őrfi, Péter Balázs Jakus, Zoltán Rumbus, Patrik Kéringer, András Garami, Eszter Vámos, Dominika Kovács, Viola Bagóné Vántus, Balázs Radnai & Tamás Lóránd
Pages: 1356-1368
Published online: 06 Jul 2021
AbstractforTetralone derivatives are MIF tautomerase inhibitors and attenuate macrophage activation and amplify the hypothermic response in endotoxemic mice | Full Text | References | PDF (3.1 MB) | EPUB | Supplemental
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Article
Design, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators
Daniel A. S. Kitagawa, Rafael B. Rodrigues, Thiago N. Silva, Wellington V. dos Santos, Vinicius C. V. da Rocha, Joyce S. F. D. de Almeida, Leandro B. Bernardo, Taynara Carvalho-Silva, Cintia N. Ferreira, Angelo A. T. da Silva, Alessandro B. C. Simas, Eugenie Nepovimova, Kamil Kuča, Tanos C. C. França & Samir F. de A. Cavalcante
Pages: 1369-1376
Published online: 21 Jun 2021
AbstractforDesign, synthesis, in silico studies and in vitro evaluation of isatin-pyridine oximes hybrids as novel acetylcholinesterase reactivators | Full Text | References | PDF (2.3 MB) | EPUB | Supplemental
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Brief Report
Novel mutual prodrug of 5-fluorouracil and heme oxygenase-1 inhibitor (5-FU/HO-1 hybrid): design and preliminary in vitro evaluation
Loredana Salerno, Luca Vanella, Valeria Sorrenti, Valeria Consoli, Valeria Ciaffaglione, Antonino N. Fallica, Vittorio Canale, Paweł Zajdel, Rosario Pignatello & Sebastiano Intagliata
Pages: 1377-1385
Published online: 24 Jun 2021
AbstractforNovel mutual prodrug of 5-fluorouracil and heme oxygenase-1 inhibitor (5-FU/HO-1 hybrid): design and preliminary in vitro evaluation | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Article
Ring size changes in the development of class I HDAC inhibitors
Er-Chieh Cho, Chi-Yuan Liu, Di-Wei Tang & Hsueh-Yun Lee
Pages: 1386-1400
Published online: 24 Jun 2021
AbstractforRing size changes in the development of class I HDAC inhibitors | PDF (2.5 MB) | Supplemental
  • 494 Views
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Brief Report
Synthesis, biological evaluation and molecular docking investigation of new sulphonamide derivatives bearing naphthalene moiety as potent tubulin polymerisation inhibitors
Guangcheng Wang, Meiyan Fan, Wenjing Liu, Min He, Yongjun Li & Zhiyun Peng
Pages: 1401-1409
Published online: 22 Jun 2021
AbstractforSynthesis, biological evaluation and molecular docking investigation of new sulphonamide derivatives bearing naphthalene moiety as potent tubulin polymerisation inhibitors | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Article
Different roles for the acyl chain and the amine leaving group in the substrate selectivity of N-Acylethanolamine acid amidase
Andrea Ghidini, Laura Scalvini, Francesca Palese, Alessio Lodola, Marco Mor & Daniele Piomelli
Pages: 1410-1422
Published online: 13 Jul 2021
AbstractforDifferent roles for the acyl chain and the amine leaving group in the substrate selectivity of N-Acylethanolamine acid amidase | Full Text | References | PDF (2.9 MB) | EPUB | Supplemental
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Article
Development of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer
Wagdy M. Eldehna, Rofaida Salem, Zainab M. Elsayed, Tarfah Al-Warhi, Hamada R. Knany, Rezk R. Ayyad, Thamer Bin Traiki, Maha-Hamadien Abdulla, Rehan Ahmad, Hatem A. Abdel-Aziz & Radwan El-Haggar
Pages: 1423-1434
Published online: 28 Jun 2021
AbstractforDevelopment of novel benzofuran-isatin conjugates as potential antiproliferative agents with apoptosis inducing mechanism in Colon cancer | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
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Design, synthesis, and biological evaluation of 5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)-1H-Indole-2-Carbohydrazide derivatives: the methuosis inducer 12A as a Novel and selective anticancer agent
Jun Wu, Hongyu Hu, Mingtao Ao, Zhenzhen Cui, Xiaoping Zhou, Jingbo Qin, Yafei Guo, Jingwei Chen, Yuhua Xue & Meijuan Fang
Pages: 1435-1452
Published online: 07 Jul 2021
AbstractforDesign, synthesis, and biological evaluation of 5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)-1H-Indole-2-Carbohydrazide derivatives: the methuosis inducer 12A as a Novel and selective anticancer agent | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
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Design and green synthesis of novel quinolinone derivatives of potential anti-breast cancer activity against MCF-7 cell line targeting multi-receptor tyrosine kinases
Mohamed Mokhtar, Khadijah S. Alghamdi, Nesreen S. Ahmed, Dina Bakhotmah & Tamer S. Saleh
Pages: 1453-1470
Published online: 01 Jul 2021
AbstractforDesign and green synthesis of novel quinolinone derivatives of potential anti-breast cancer activity against MCF-7 cell line targeting multi-receptor tyrosine kinases | Full Text | References | PDF (4.4 MB) | EPUB | Supplemental
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Anti-tubercular activity and molecular docking studies of indolizine derivatives targeting mycobacterial InhA enzyme
Katharigatta N. Venugopala, Sandeep Chandrashekharappa, Pran Kishore Deb, Christophe Tratrat, Melendhran Pillay, Deepak Chopra, Nizar A. Al-Shar’i, Wafa Hourani, Lina A. Dahabiyeh, Pobitra Borah, Rahul D. Nagdeve, Susanta K. Nayak, Basavaraj Padmashali, Mohamed A. Morsy, Bandar E. Aldhubiab, Mahesh Attimarad, Anroop B. Nair, Nagaraja Sreeharsha, Michelyne Haroun, Sheena Shashikanth, Viresh Mohanlall & Raghuprasad Mailavaram
Pages: 1471-1486
Published online: 01 Jul 2021
AbstractforAnti-tubercular activity and molecular docking studies of indolizine derivatives targeting mycobacterial InhA enzyme | Full Text | References | PDF (4.1 MB) | EPUB | Supplemental
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Design, synthesis, and analysis of antiproliferative and apoptosis-inducing activities of nitrile derivatives containing a benzofuran scaffold: EGFR inhibition assay and molecular modelling study
Salma Fares, Khalid B. Selim, Fatma E. Goda, Magda A. A. El-Sayed, Nawaf A. AlSaif, Mohamed M. Hefnawy, Alaa A.-M. Abdel-Aziz & Adel S. El-Azab
Pages: 1487-1498
Published online: 06 Jul 2021
AbstractforDesign, synthesis, and analysis of antiproliferative and apoptosis-inducing activities of nitrile derivatives containing a benzofuran scaffold: EGFR inhibition assay and molecular modelling study | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
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Synthesis and evaluation of AKR1C inhibitory properties of A-ring halogenated oestrone derivatives
Maša Sinreih, Rebeka Jójárt, Zoltán Kele, Tomaž Büdefeld, Gábor Paragi, Erzsébet Mernyák & Tea Lanišnik Rižner
Pages: 1499-1507
Published online: 06 Jul 2021
AbstractforSynthesis and evaluation of AKR1C inhibitory properties of A-ring halogenated oestrone derivatives | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
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Diaryl azo derivatives as anti-diabetic and antimicrobial agents: synthesis, in vitro, kinetic and docking studies
Tehreem Tahir, Mirza Imran Shahzad, Rukhsana Tabassum, Muhammad Rafiq, Muhammad Ashfaq, Mubashir Hassan, Katarzyna Kotwica-Mojzych & Mariusz Mojzych
Pages: 1508-1519
Published online: 08 Jul 2021
AbstractforDiaryl azo derivatives as anti-diabetic and antimicrobial agents: synthesis, in vitro, kinetic and docking studies | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Synthesis, potential antitumor activity, cell cycle analysis, and multitarget mechanisms of novel hydrazones incorporating a 4-methylsulfonylbenzene scaffold: a molecular docking study
Alaa A.-M. Abdel-Aziz, Adel S. El-Azab, Nawaf A. AlSaif, Ahmad J. Obaidullah, Abdulrahman M. Al-Obaid & Ibrahim A. Al-Suwaidan
Pages: 1520-1538
Published online: 15 Jul 2021
AbstractforSynthesis, potential antitumor activity, cell cycle analysis, and multitarget mechanisms of novel hydrazones incorporating a 4-methylsulfonylbenzene scaffold: a molecular docking study | Full Text | References | PDF (3.7 MB) | EPUB | Supplemental
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Identification of imidazo[4,5-c]pyridin-2-one derivatives as novel Src family kinase inhibitors against glioblastoma
Lishun Zhang, Zichao Yang, Huiting Sang, Ying Jiang, Mingfeng Zhou, Chuan Huang, Chunhui Huang, Xiaoyun Wu, Tingting Zhang, Xingmei Zhang, Shanhe Wan & Jiajie Zhang
Pages: 1539-1550
Published online: 08 Jul 2021
AbstractforIdentification of imidazo[4,5-c]pyridin-2-one derivatives as novel Src family kinase inhibitors against glioblastoma | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
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Design, synthesis, HER2 inhibition and anticancer evaluation of new substituted 1,5-dihydro-4,1-benzoxazepines
Olga Cruz-López, Matilde Ner, Francho Nerín-Fonz, Yaiza Jiménez-Martínez, David Araripe, Juan A. Marchal, Houria Boulaiz, Hugo Gutiérrez-de-Terán, Joaquín M. Campos & Ana Conejo-García
Pages: 1551-1561
Published online: 12 Jul 2021
AbstractforDesign, synthesis, HER2 inhibition and anticancer evaluation of new substituted 1,5-dihydro-4,1-benzoxazepines | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Tertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer
Lijuan Ding, Feng Wei, Nanya Wang, Yue Sun, Qiang Wang, Xia Fan, Ling Qi & Shudong Wang
Pages: 1562-1571
Published online: 19 Jul 2021
AbstractforTertiary sulphonamide derivatives as dual acting small molecules that inhibit LSD1 and suppress tubulin polymerisation against liver cancer | Full Text | References | PDF (2.4 MB) | EPUB | Supplemental
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New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011–2021) focussing on structure–activity relationship (SAR) and docking insights
Ahmed Elkamhawy, Eslam M. H. Ali & Kyeong Lee
Pages: 1572-1600
Published online: 07 Jul 2021
AbstractforNew horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011–2021) focussing on structure–activity relationship (SAR) and docking insights | Full Text | References | PDF (5.9 MB) | EPUB
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Brief Report
CO2 permeability of the rat erythrocyte membrane and its inhibition
Samer Al-Samir, Maximilian Prill, Claudiu T. Supuran, Gerolf Gros & Volker Endeward
Pages: 1601-1605
Published online: 14 Jul 2021
AbstractforCO2 permeability of the rat erythrocyte membrane and its inhibition | Full Text | References | PDF (859.6 KB) | EPUB
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Sheunopa C. Mzezewa, Sylvester I. Omoruyi, Luke S. Zondagh, Sarel F. Malan, Okobi E. Ekpo & Jacques Joubert
Pages: 1606-1620
Published online: 19 Jul 2021
AbstractforDesign, synthesis, and evaluation of 3,7-substituted coumarin derivatives as multifunctional Alzheimer’s disease agents | Full Text | References | PDF (2.9 MB) | EPUB
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Trifluoromethyl-substituted 3,5-bis(arylidene)-4-piperidones as potential anti-hepatoma and anti-inflammation agents by inhibiting NF-кB activation
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Pages: 1621-1630
Published online: 20 Jul 2021
AbstractforTrifluoromethyl-substituted 3,5-bis(arylidene)-4-piperidones as potential anti-hepatoma and anti-inflammation agents by inhibiting NF-кB activation | Full Text | References | PDF (2 MB) | EPUB | Supplemental
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New azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study
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Published online: 21 Jul 2021
AbstractforNew azolyl-derivatives as multitargeting agents against breast cancer and fungal infections: synthesis, biological evaluation and docking study | Full Text | References | PDF (3.5 MB) | EPUB | Supplemental
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Supervised Molecular Dynamics (SuMD) Insights into the mechanism of action of SARS-CoV-2 main protease inhibitor PF-07321332
Matteo Pavan, Giovanni Bolcato, Davide Bassani, Mattia Sturlese & Stefano Moro
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Published online: 21 Jul 2021
AbstractforSupervised Molecular Dynamics (SuMD) Insights into the mechanism of action of SARS-CoV-2 main protease inhibitor PF-07321332 | Full Text | References | PDF (1.2 MB) | EPUB | Supplemental
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Strained contacts with the cell membrane may influence ligand affinity to G protein coupled receptors: a case of free fatty acid receptor 1 agonists
Alexey Lukin, Anna Bakholdina, Mikhail Chudinov, Oleksandra Onopchenko, Elena Zhuravel, Sergey Zozulya, Maxim Gureev & Mikhail Krasavin
Pages: 1650-1657
Published online: 22 Jul 2021
AbstractforStrained contacts with the cell membrane may influence ligand affinity to G protein coupled receptors: a case of free fatty acid receptor 1 agonists | Full Text | References | PDF (2.7 MB) | EPUB
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Tereza Cristina Santos Evangelista, Óscar López, Sabrina Baptista Ferreira, José G. Fernández-Bolaños, Magne O. Sydnes & Emil Lindbäck
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Published online: 22 Jul 2021
AbstractforDevelopment of tacrine clusters as positively cooperative systems for the inhibition of acetylcholinesterase | Full Text | References | PDF (1,015.6 KB) | Supplemental
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Hao He, Huifang Li, Toyosi Akanji, Shengli Niu, Zhujun Luo, Dongli Li, Navindra P. Seeram, Panpan Wu & Hang Ma
Pages: 1664-1677
Published online: 26 Jul 2021
AbstractforSynthesis and biological evaluations of oleanolic acid indole derivatives as hyaluronidase inhibitors with enhanced skin permeability | Full Text | References | PDF (3.4 MB) | EPUB
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The role of mTOR in age-related diseases
Zofia Chrienova, Eugenie Nepovimova & Kamil Kuca
Pages: 1678-1692
Published online: 26 Jul 2021
AbstractforThe role of mTOR in age-related diseases | Full Text | References | PDF (1.9 MB) | EPUB
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Brief Report
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Guangcheng Wang, Wenjing Liu, Meiyan Fan, Min He, Yongjun Li & Zhiyun Peng
Pages: 1693-1701
Published online: 26 Jul 2021
AbstractforDesign, synthesis and biological evaluation of novel thiazole-naphthalene derivatives as potential anticancer agents and tubulin polymerisation inhibitors | Full Text | References | PDF (2.8 MB) | EPUB | Supplemental
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Multitargeting approaches involving carbonic anhydrase inhibitors: hybrid drugs against a variety of disorders
Claudiu T. Supuran
Pages: 1702-1714
Published online: 30 Jul 2021
AbstractforMultitargeting approaches involving carbonic anhydrase inhibitors: hybrid drugs against a variety of disorders | Full Text | References | PDF (2.3 MB)
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Discovery of N-aryl sulphonamide-quinazoline derivatives as anti-gastric cancer agents in vitro and in vivo via activating the Hippo signalling pathway
Jin-Bo Niu, Chun-Hua Quan, Yuan Liu, Guang-Xi Yu, Jia-Jia Yang, Yin-Ru Li, Yan-Bing Zhang, Ying-Qiu Qi, Jian Song, Cheng-Yun Jin & Sai-Yang Zhang
Pages: 1715-1731
Published online: 23 Aug 2021
AbstractforDiscovery of N-aryl sulphonamide-quinazoline derivatives as anti-gastric cancer agents in vitro and in vivo via activating the Hippo signalling pathway | Full Text | References | PDF (4.5 MB) | EPUB | Supplemental
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Discovery of new 3-methylquinoxalines as potential anti-cancer agents and apoptosis inducers targeting VEGFR-2: design, synthesis, and in silico studies
Mohammed M. Alanazi, Alaa Elwan, Nawaf A. Alsaif, Ahmad J. Obaidullah, Hamad M. Alkahtani, Abdulrahman A. Al-Mehizia, Sultan M. Alsubaie, Mohammed S. Taghour & Ibrahim H. Eissa
Pages: 1732-1750
Published online: 29 Jul 2021
AbstractforDiscovery of new 3-methylquinoxalines as potential anti-cancer agents and apoptosis inducers targeting VEGFR-2: design, synthesis, and in silico studies | Full Text | References | PDF (4.5 MB) | EPUB
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Design and characterisation of piperazine-benzofuran integrated dinitrobenzenesulfonamide as Mycobacterium tuberculosis H37Rv strain inhibitors
Vallabhaneni S. Murthy, Yasinalli Tamboli, Vagolu Siva Krishna, Dharmarajan Sriram, Siddique Akber Ansari, Abdullah A. Alarfaj, Abdurahman H. Hirad & Vijayaparthasarathi Vijayakumar
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Published online: 29 Jul 2021
AbstractforDesign and characterisation of piperazine-benzofuran integrated dinitrobenzenesulfonamide as Mycobacterium tuberculosis H37Rv strain inhibitors | Full Text | References | PDF (2.2 MB) | EPUB | Supplemental
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Design, synthesis, docking, ADMET studies, and anticancer evaluation of new 3-methylquinoxaline derivatives as VEGFR-2 inhibitors and apoptosis inducers
Mohammed M. Alanazi, Ibrahim H. Eissa, Nawaf A. Alsaif, Ahmad J. Obaidullah, Wael A. Alanazi, Abdullah F. Alasmari, Hussam Albassam, Hazem Elkady & Alaa Elwan
Pages: 1760-1782
Published online: 02 Aug 2021
AbstractforDesign, synthesis, docking, ADMET studies, and anticancer evaluation of new 3-methylquinoxaline derivatives as VEGFR-2 inhibitors and apoptosis inducers | Full Text | References | PDF (4.2 MB) | EPUB
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Carbonic anhydrase activation profile of indole-based derivatives
Elisabetta Barresi, Rahul Ravichandran, Lorenzo Germelli, Andrea Angeli, Emma Baglini, Silvia Salerno, Anna Maria Marini, Barbara Costa, Eleonora Da Pozzo, Claudia Martini, Federico Da Settimo, Claudiu Supuran, Sandro Cosconati & Sabrina Taliani
Pages: 1783-1797
Published online: 02 Aug 2021
AbstractforCarbonic anhydrase activation profile of indole-based derivatives | Full Text | References | PDF (3.3 MB) | EPUB
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Identifying requirements for RSK2 specific inhibitors
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Pages: 1798-1809
Published online: 05 Aug 2021
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Design and synthesis of novel quinazolinones conjugated ibuprofen, indole acetamide, or thioacetohydrazide as selective COX-2 inhibitors: anti-inflammatory, analgesic and anticancer activities
Asmaa Sakr, Samar Rezq, Samy M. Ibrahim, Eman Soliman, Mohamed M. Baraka, Damian G. Romero & Hend Kothayer
Pages: 1810-1828
Published online: 01 Aug 2021
AbstractforDesign and synthesis of novel quinazolinones conjugated ibuprofen, indole acetamide, or thioacetohydrazide as selective COX-2 inhibitors: anti-inflammatory, analgesic and anticancer activities | Full Text | References | PDF (3 MB) | EPUB | Supplemental
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Cyanobacteria and microalgae bioactive compounds in skin-ageing: potential to restore extracellular matrix filling and overcome hyperpigmentation
Rita Favas, Janaína Morone, Rosário Martins, Vitor Vasconcelos & Graciliana Lopes
Pages: 1829-1838
Published online: 06 Aug 2021
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New benzothieno[2,3-c]pyridines as non-steroidal CYP17 inhibitors: design, synthesis, anticancer screening, apoptosis induction, and in silico ADME profile studies
Nadia A. Khalil, Eman M. Ahmed, Ashraf F. Zaher, Eman A. Sobh, Samiha A. El-Sebaey & Mona S. El-Zoghbi
Pages: 1839-1859
Published online: 02 Aug 2021
AbstractforNew benzothieno[2,3-c]pyridines as non-steroidal CYP17 inhibitors: design, synthesis, anticancer screening, apoptosis induction, and in silico ADME profile studies | Full Text | References | PDF (3.3 MB) | EPUB | Supplemental
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Structure–activity relationship, in vitro and in vivo evaluation of novel dienyl sulphonyl fluorides as selective BuChE inhibitors for the treatment of Alzheimer's disease
Chengyao Wu, Guijuan Zhang, Zai-Wei Zhang, Xia Jiang, Ziwen Zhang, Huanhuan Li, Hua-Li Qin & Wenjian Tang
Pages: 1860-1873
Published online: 23 Aug 2021
AbstractforStructure–activity relationship, in vitro and in vivo evaluation of novel dienyl sulphonyl fluorides as selective BuChE inhibitors for the treatment of Alzheimer's disease | Full Text | References | PDF (3.2 MB) | EPUB | Supplemental
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Tetrahydroquinazole-based secondary sulphonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IV, and IX, and computational studies
Emma Baglini, Rahul Ravichandran, Emanuela Berrino, Silvia Salerno, Elisabetta Barresi, Anna Maria Marini, Monica Viviano, Sabrina Castellano, Federico Da Settimo, Claudiu T. Supuran, Sandro Cosconati & Sabrina Taliani
Pages: 1874-1883
Published online: 02 Aug 2021
AbstractforTetrahydroquinazole-based secondary sulphonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IV, and IX, and computational studies | Full Text | References | PDF (2.9 MB) | EPUB
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Synthesis and anti-hepatocellular carcinoma activity of aminopyridinol–sorafenib hybrids
Bhuwan Prasad Awasthi, Prakash Chaudhary, Diwakar Guragain, Jun-Goo Jee, Jung-Ae Kim & Byeong-Seon Jeong
Pages: 1884-1897
Published online: 02 Aug 2021
AbstractforSynthesis and anti-hepatocellular carcinoma activity of aminopyridinol–sorafenib hybrids | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Anticancer activity and toxicity of new quaternary ammonium geldanamycin derivative salts and their mixtures with potentiators
Natalia Skrzypczak, Krystian Pyta, Piotr Ruszkowski, Przemysław Mikołajczak, Małgorzata Kucińska, Marek Murias, Maria Gdaniec, Franz Bartl & Piotr Przybylski
Pages: 1898-1904
Published online: 04 Aug 2021
AbstractforAnticancer activity and toxicity of new quaternary ammonium geldanamycin derivative salts and their mixtures with potentiators | Full Text | References | PDF (1.4 MB) | EPUB | Supplemental
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Dual inhibition of EGFR and IL-6-STAT3 signalling by miR-146b: a potential targeted therapy for epithelial ovarian cancer
Meina Yan, Mutian Han, Xinxin Yang, Rong Shen, Hui Wang, Lubin Zhang, Sheng Xia, Peifang Yang, Guanghua Zhai & Qixiang Shao
Pages: 1905-1915
Published online: 08 Aug 2021
AbstractforDual inhibition of EGFR and IL-6-STAT3 signalling by miR-146b: a potential targeted therapy for epithelial ovarian cancer | Full Text | References | PDF (3.6 MB) | EPUB | Supplemental
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Brief Report
Three-component Castagnoli-Cushman reaction with ammonium acetate delivers 2-unsubstituted isoquinol-1-ones as potent inhibitors of poly(ADP-ribose) polymerase (PARP)
Alexander Safrygin, Petr Zhmurov, Dmitry Dar’in, Sergey Silonov, Mariia Kasatkina, Yulia Zonis, Maxim Gureev & Mikhail Krasavin
Pages: 1916-1921
Published online: 31 Aug 2021
AbstractforThree-component Castagnoli-Cushman reaction with ammonium acetate delivers 2-unsubstituted isoquinol-1-ones as potent inhibitors of poly(ADP-ribose) polymerase (PARP) | Full Text | References | PDF (1.4 MB) | EPUB
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Pyrrolidine-based 3-deoxysphingosylphosphorylcholine analogs as possible candidates against neglected tropical diseases (NTDs): identification of hit compounds towards development of potential treatment of Leishmania donovani
Ahmed H. E. Hassan, Trong-Nhat Phan, Seolmin Yoon, Cheol Jung Lee, Hye Rim Jeon, Seung-Hwan Kim, Joo Hwan No & Yong Sup Lee
Pages: 1922-1930
Published online: 23 Aug 2021
AbstractforPyrrolidine-based 3-deoxysphingosylphosphorylcholine analogs as possible candidates against neglected tropical diseases (NTDs): identification of hit compounds towards development of potential treatment of Leishmania donovani | Full Text | References | PDF (1.7 MB) | EPUB | Supplemental
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Microwave-assisted Phospha-Michael addition reactions in the 13α-oestrone series and in vitro antiproliferative properties
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Pages: 1931-1937
Published online: 27 Aug 2021
AbstractforMicrowave-assisted Phospha-Michael addition reactions in the 13α-oestrone series and in vitro antiproliferative properties | Full Text | References | PDF (979.8 KB) | EPUB | Supplemental
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In vitro and in silico studies of bis (indol-3-yl) methane derivatives as potential α-glucosidase and α-amylase inhibitors
Peng-Fei Zheng, Zhuang Xiong, Cui-ying Liao, Xin Zhang, Mei Feng, Xiao-Zheng Wu, Jing Lin, Lin-Sheng Lei, You-Cheng Zhang, Shao-Hua Wang & Xue-Tao Xu
Pages: 1938-1951
Published online: 30 Aug 2021
AbstractforIn vitro and in silico studies of bis (indol-3-yl) methane derivatives as potential α-glucosidase and α-amylase inhibitors | Full Text | References | PDF (2.4 MB) | EPUB
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Synthesis, antiproliferative and antitrypanosomal activities, and DNA binding of novel 6-amidino-2-arylbenzothiazoles
Livio Racané, Valentina Rep, Sandra Kraljević Pavelić, Petra Grbčić, Iva Zonjić, Marijana Radić Stojković, Martin C. Taylor, John M. Kelly & Silvana Raić-Malić
Pages: 1952-1967
Published online: 30 Aug 2021
AbstractforSynthesis, antiproliferative and antitrypanosomal activities, and DNA binding of novel 6-amidino-2-arylbenzothiazoles | Full Text | References | PDF (5.4 MB) | EPUB | Supplemental
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Brief Report
1-Oxo-3,4-dihydroisoquinoline-4-carboxamides as novel druglike inhibitors of poly(ADP-ribose) polymerase (PARP) with favourable ADME characteristics
Alexander Safrygin, Petr Zhmurov, Dmitry Dar’in, Sergey Silonov, Mariia Kasatkina, Yulia Zonis, Maxim Gureev & Mikhail Krasavin
Pages: 1968-1983
Published online: 06 Sep 2021
Abstractfor1-Oxo-3,4-dihydroisoquinoline-4-carboxamides as novel druglike inhibitors of poly(ADP-ribose) polymerase (PARP) with favourable ADME characteristics | Full Text | References | PDF (4.2 MB) | EPUB | Supplemental
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Correction
Correction
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Published online: 06 Sep 2021
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An overview on the recently discovered iota-carbonic anhydrases
Alessio Nocentini, Claudiu T. Supuran & Clemente Capasso
Pages: 1988-1995
Published online: 06 Sep 2021
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Pages: 1996-2009
Published online: 15 Sep 2021
AbstractforDiscovery of facile amides-functionalized rhodanine-3-acetic acid derivatives as potential anticancer agents by disrupting microtubule dynamics | Full Text | References | PDF (2.7 MB) | EPUB
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The possible role of methylglyoxal metabolism in cancer
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Pages: 2010-2015
Published online: 13 Sep 2021
AbstractforThe possible role of methylglyoxal metabolism in cancer | Full Text | References | PDF (1.2 MB) | EPUB
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High-yield synthesis and purification of recombinant human GABA transaminase for high-throughput screening assays
Mingu Gordon Park, Ah-reum Han, Su Yeon Kim, Tai Young Kim, Ho Min Kim & C. Justin Lee
Pages: 2016-2024
Published online: 12 Sep 2021
AbstractforHigh-yield synthesis and purification of recombinant human GABA transaminase for high-throughput screening assays | Full Text | References | PDF (2.9 MB) | EPUB
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Alba Vicente-Blázquez, Myriam González, Manuel Medarde, Faustino Mollinedo & Rafael Peláez
Pages: 2025-2044
Published online: 12 Sep 2021
AbstractforNew indolesulfonamide derivatives targeting the colchicine site of tubulin: synthesis, anti-tumour activity, structure–activity relationships, and molecular modelling | PDF (3.5 MB) | Supplemental
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Xiaoying Jiang, Jianan Guo, Changjun Zhang, Jinping Gu, Tao Zhou, Renren Bai & Yuanyuan Xie
Pages: 2045-2054
Published online: 04 Oct 2021
AbstractforDiscovery of benzamide-hydroxypyridinone hybrids as potent multi-targeting agents for the treatment of Alzheimer's disease | Full Text | References | PDF (2.6 MB) | EPUB | Supplemental
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Quinazolin-4(3H)-one based potential multiple tyrosine kinase inhibitors with excellent cytotoxicity
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Published online: 22 Sep 2021
AbstractforQuinazolin-4(3H)-one based potential multiple tyrosine kinase inhibitors with excellent cytotoxicity | Full Text | References | PDF (2.5 MB) | EPUB | Supplemental
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Carnitine is a pharmacological allosteric chaperone of the human lysosomal α-glucosidase
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Published online: 27 Sep 2021
AbstractforCarnitine is a pharmacological allosteric chaperone of the human lysosomal α-glucosidase | Full Text | References | PDF (2.7 MB) | EPUB | Supplemental
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Inhibitors of histone deacetylase 6 based on a novel 3-hydroxy-isoxazole zinc binding group
Pasquale Linciano, Luca Pinzi, Silvia Belluti, Ugo Chianese, Rosaria Benedetti, Davide Moi, Lucia Altucci, Silvia Franchini, Carol Imbriano, Claudia Sorbi & Giulio Rastelli
Pages: 2080-2086
Published online: 28 Sep 2021
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Zhe Zhang, Zhao-Sheng Zhang, Xiao Wang, Gao-Lei Xi, Zhen Jin & You-Zhi Tang
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Published online: 25 Nov 2021
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Recent advance in the discovery of tyrosinase inhibitors from natural sources via separation methods
Xiao-wei Zhang, Guang-li Bian, Pei-ying Kang, Xin-jie Cheng, Kai Yan, Yong-li Liu, Yan-xia Gao & De-qiang Li
Pages: 2104-2117
Published online: 27 Sep 2021
AbstractforRecent advance in the discovery of tyrosinase inhibitors from natural sources via separation methods | Full Text | References | PDF (1.9 MB) | EPUB | Supplemental
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Leonardo E. Riafrecha, Macarena S. Le Pors, Martín J. Lavecchia, Silvia Bua, Claudiu T. Supuran & Pedro A. Colinas
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Published online: 04 Oct 2021
AbstractforVanillin enones as selective inhibitors of the cancer associated carbonic anhydrase isoforms IX and XII. The out of the active site pocket for the design of selective inhibitors? | Full Text | References | PDF (2.1 MB) | EPUB | Supplemental
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Francesco Fiorentino, Marta De Angelis, Martina Menna, Annarita Rovere, Anna Maria Caccuri, Francesca D’Acunzo, Anna Teresa Palamara, Lucia Nencioni, Dante Rotili & Antonello Mai
Pages: 2128-2138
Published online: 28 Sep 2021
AbstractforAnti-influenza A virus activity and structure–activity relationship of a series of nitrobenzoxadiazole derivatives | Full Text | References | PDF (4.4 MB) | EPUB | Supplemental
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Small molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review
Ming Bian, Qian-qian Ma, Yun Wu, Huan-huan Du & Gong Guo-hua
Pages: 2139-2159
Published online: 11 Oct 2021
AbstractforSmall molecule compounds with good anti-inflammatory activity reported in the literature from 01/2009 to 05/2021: a review | Full Text | References | PDF (2.7 MB) | EPUB
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Published online: 30 Sep 2021
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Rongshuang Luo, Zhongyuan Wang, Dali Luo, Yumei Qin, Chunshen Zhao, Di Yang, Tian Lu, Zhixu Zhou & Zhuyan Huang
Pages: 2170-2182
Published online: 08 Nov 2021
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Pages: 2183-2198
Published online: 04 Oct 2021
AbstractforSynthesis of novel pyrroles and fused pyrroles as antifungal and antibacterial agents | Full Text | References | PDF (1.5 MB) | EPUB | Supplemental
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