1, 2, 3-Triazole analogs of combretastatin A-4 as potential microtubule-binding agents

K Odlo, J Fournier-Dit-Chabert, S Ducki…

Index: Odlo, Kristin; Fournier-Dit-Chabert, Jeremie; Ducki, Sylvie; Gani, Osman A.B.S.M.; Sylte, Ingebrigt; Hansen, Trond Vidar Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 18 p. 6874 - 6885

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Citation Number: 54

Abstract

A series of cis-restricted 1, 4-and 1, 5-disubstituted 1, 2, 3-triazole analogs of combretastatin A-4 (1) have been prepared. Cytotoxicity and tubulin inhibition studies showed that 2- methoxy-5-((5-(3, 4, 5-trimethoxyphenyl)-1H-1, 2, 3-triazol-1-yl) methyl) aniline (5e) and 2- methoxy-5-(1-(3, 4, 5-trimethoxybenzyl)-1H-1, 2, 3-triazol-5-yl) aniline (6e) were two of the most active compounds. Molecular modeling studies revealed that the N-2 and N-3 atoms ...

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