Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 30, Issue 5 (2015)

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Journal of Enzyme Inhibition and Medicinal Chemistry, Volume 30, Issue 5 (2015)

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Review Article

Targeting tumour hypoxia to prevent cancer metastasis. From biology, biosensing and technology to drug development: the METOXIA consortium
Erik O. Pettersen, Peter Ebbesen, Roben G. Gieling, Kaye J. Williams, Ludwig Dubois, Philippe Lambin, Carol Ward, James Meehan, Ian H. Kunkler, Simon P. Langdon, Anne H. Ree, Kjersti Flatmark, Heidi Lyng, Maria J. Calzada, Luis del Peso, Manuel O. Landazuri, Agnes Görlach, Hubert Flamm, Jochen Kieninger, Gerald Urban, Andreas Weltin, Dean C. Singleton, Syed Haider, Francesca M. Buffa, Adrian L. Harris, Andrea Scozzafava, Claudiu T. Supuran, Isabella Moser, Gerhard Jobst, Morten Busk, Kasper Toustrup, Jens Overgaard, Jan Alsner, Jacques Pouyssegur, Johanna Chiche, Nathalie Mazure, Ibtissam Marchiq, Scott Parks, Afshan Ahmed, Margaret Ashcroft, Silvia Pastorekova, Yihai Cao, Kasper M. Rouschop, Brad G. Wouters, Marianne Koritzinsky, Hilda Mujcic & Dan Cojocari
Pages: 689-721
Published online: 27 Oct 2014
AbstractforTargeting tumour hypoxia to prevent cancer metastasis. From biology, biosensing and technology to drug development: the METOXIA consortium | Full Text | References | PDF (2.5 MB)
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Research Article

Article
Effective attenuation of atrazine-induced histopathological changes in testicular tissue by antioxidant N-phenyl-4-aryl-polyhydroquinolines
Navneet Chandak, Jitender K. Bhardwaj, Dimitrina Zheleva-Dimitrova, Gerassim Kitanov, Rajnesh K. Sharma, Pawan K. Sharma & Luciano Saso
Pages: 722-729
Published online: 27 Aug 2015
AbstractforEffective attenuation of atrazine-induced histopathological changes in testicular tissue by antioxidant N-phenyl-4-aryl-polyhydroquinolines | Full Text | References | PDF (1,004 KB) | Supplemental
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Original Article

Article
Design, synthesis and evaluation of 2,4-diarylpyrano[3,2-c]chromen-5(4H)-one as a new class of non-purine xanthine oxidase inhibitors
Harpreet S. Virdi, Sahil Sharma, Samir Mehndiratta, P. M. S. Bedi & Kunal Nepali
Pages: 730-736
Published online: 27 Aug 2015
AbstractforDesign, synthesis and evaluation of 2,4-diarylpyrano[3,2-c]chromen-5(4H)-one as a new class of non-purine xanthine oxidase inhibitors | Full Text | References | PDF (1.3 MB) | Supplemental
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Research Article

Article
Fluorinated pyrrolidines and piperidines incorporating tertiary benzenesulfonamide moieties are selective carbonic anhydrase II inhibitors
Alexandre Le Darz, Agnès Mingot, Fodil Bouazza, Ugo Castelli, Omar Karam, Muhammet Tanc, Claudiu T. Supuran & Sébastien Thibaudeau
Pages: 737-745
Published online: 28 Nov 2014
AbstractforFluorinated pyrrolidines and piperidines incorporating tertiary benzenesulfonamide moieties are selective carbonic anhydrase II inhibitors | Full Text | References | PDF (640 KB)
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Article
Synthesis, central nervous system activity and structure–activity relationship of N-substituted derivatives of 1-arylimidazolidyn-2-ylideneurea and products of their cyclization
Elżbieta Szacoń, Marzena Rządkowska, Agnieszka A. Kaczor, Ewa Kędzierska, Antonina Mazur, Sylwia Fidecka & Dariusz Matosiuk
Pages: 746-760
Published online: 11 Feb 2015
AbstractforSynthesis, central nervous system activity and structure–activity relationship of N-substituted derivatives of 1-arylimidazolidyn-2-ylideneurea and products of their cyclization | Full Text | References | PDF (1.5 MB)
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Article
Acethylcholinesterase inhibitory potential and antioxidant properties of pyrogallol
S. Beyza Ozturk Sarikaya
Pages: 761-766
Published online: 27 Aug 2015
AbstractforAcethylcholinesterase inhibitory potential and antioxidant properties of pyrogallol | Full Text | References | PDF (203.8 KB) | Supplemental
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Article
Carbamoylphosphonates inhibit autotaxin and metastasis formation in vivo
Reuven Reich, Amnon Hoffman, R. Rama Suresh, Ofra Shai, Julia Frant, Alfonso Maresca, Claudiu T. Supuran & Eli Breuer
Pages: 767-772
Published online: 11 Feb 2015
AbstractforCarbamoylphosphonates inhibit autotaxin and metastasis formation in vivo | Full Text | References | PDF (811.1 KB)
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Article
7-Amino-3,4-dihydro-1H-quinolin-2-one, a compound similar to the substituted coumarins, inhibits α-carbonic anhydrases without hydrolysis of the lactam ring
Daniela Vullo, Semra Isik, Murat Bozdag, Fabrizio Carta & Claudiu T. Supuran
Pages: 773-777
Published online: 12 Feb 2015
Abstractfor7-Amino-3,4-dihydro-1H-quinolin-2-one, a compound similar to the substituted coumarins, inhibits α-carbonic anhydrases without hydrolysis of the lactam ring | Full Text | References | PDF (246.7 KB)
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Article
Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles
Pelin Çıkla-Süzgün, Neerja Kaushik-Basu, Amartya Basu, Payal Arora, Tanaji T. Talele, Irem Durmaz, Rengül Çetin-Atalay & Ş.Güniz Küçükgüzel
Pages: 778-785
Published online: 27 Aug 2015
AbstractforAnti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles | Full Text | References | PDF (545.2 KB) | Supplemental
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Article
Novel thiosemicarbazides induced apoptosis in human MCF-7 breast cancer cells via JNK signaling
Ahmed Malki, Rasha Y. Elbayaa, Hayam M.A. Ashour, Christopher A. Loffredo & Amal M. Youssef
Pages: 786-795
Published online: 27 Aug 2015
AbstractforNovel thiosemicarbazides induced apoptosis in human MCF-7 breast cancer cells via JNK signaling | Full Text | References | PDF (1,018.8 KB) | Supplemental
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Article
Evaluation of 2,6-dichlorophenolindophenol acetate as a substrate for acetylcholinesterase activity assay
Miroslav Pohanka & Ondrej Holas
Pages: 796-799
Published online: 12 Feb 2015
AbstractforEvaluation of 2,6-dichlorophenolindophenol acetate as a substrate for acetylcholinesterase activity assay | Full Text | References | PDF (371.6 KB)
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Article
Design, synthesis and in vitro bactericidal/fungicidal screening of some vanadyl(IV)complexes with mono- and di-substituted ONS donor triazoles
Sajjad H. Sumrra, Muhammad Hanif & Zahid H. Chohan
Pages: 800-808
Published online: 26 Feb 2015
AbstractforDesign, synthesis and in vitro bactericidal/fungicidal screening of some vanadyl(IV)complexes with mono- and di-substituted ONS donor triazoles | Full Text | References | PDF (826.1 KB)
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Article
Compressed images for affinity prediction-2 (CIFAP-2): an improved machine learning methodology on protein–ligand interactions based on a study on caspase 3 inhibitors
Ozlem Erdas, Cenk. A. Andac, A. Selen Gurkan-Alp, Ferda Nur Alpaslan & Erdem Buyukbingol
Pages: 809-815
Published online: 27 Aug 2015
AbstractforCompressed images for affinity prediction-2 (CIFAP-2): an improved machine learning methodology on protein–ligand interactions based on a study on caspase 3 inhibitors | Full Text | References | PDF (380.4 KB) | Supplemental
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Article
Synthesis and anti-cancer activity evaluation of new aurone derivatives
Seref Demirayak, Leyla Yurttas, Nalan Gundogdu-Karaburun, Ahmet Cagri Karaburun & Ismail Kayagil
Pages: 816-825
Published online: 27 Aug 2015
AbstractforSynthesis and anti-cancer activity evaluation of new aurone derivatives | Full Text | References | PDF (494.1 KB) | Supplemental
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Article
Synthesis, in vitro and in vivo antitumor and antiviral activity of novel 1-substituted benzimidazole derivatives
Yasser M. Shaker, Mohamed A. Omar, Khaled Mahmoud, Salwa M. Elhallouty, Waled M. El-Senousy, Mamdouh M. Ali, Abeer E. Mahmoud, Abeer H. Abdel-Halim, Saeed M. Soliman & Hoda I. El Diwani
Pages: 826-845
Published online: 27 Aug 2015
AbstractforSynthesis, in vitro and in vivo antitumor and antiviral activity of novel 1-substituted benzimidazole derivatives | Full Text | References | PDF (3.3 MB) | Supplemental
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Short Communication

Chiral resolution, determination of absolute configuration, and biological evaluation of (1,2-benzothiazin-4-yl)acetic acid enantiomers as aldose reductase inhibitors
Xin Hao, Xiangyu Qin, Saghir Hussain, Shagufta Parveen, Wei Zhang, Fengyan Fu, Bing Ma & Changjin Zhu
Pages: 846-851
Published online: 27 Aug 2015
AbstractforChiral resolution, determination of absolute configuration, and biological evaluation of (1,2-benzothiazin-4-yl)acetic acid enantiomers as aldose reductase inhibitors | Full Text | References | PDF (897.1 KB) | Supplemental
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In vitro neuroprotective activity of sesquiterpenoids from the flower buds of Tussilago farfara
Hyo Jin Lim, Guang-zhi Dong, Hwa Jin Lee & Jae-Ha Ryu
Pages: 852-856
Published online: 07 Oct 2014
AbstractforIn vitro neuroprotective activity of sesquiterpenoids from the flower buds of Tussilago farfara | Full Text | References | PDF (405 KB)
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C-glycosides incorporating the 6-methoxy-2-naphthyl moiety are selective inhibitors of fungal and bacterial carbonic anhydrases
Leonardo E. Riafrecha, Daniela Vullo, Claudiu T. Supuran & Pedro A. Colinas
Pages: 857-861
Published online: 07 Oct 2014
AbstractforC-glycosides incorporating the 6-methoxy-2-naphthyl moiety are selective inhibitors of fungal and bacterial carbonic anhydrases | Full Text | References | PDF (193.3 KB)
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