Please use this identifier to cite or link to this item: http://hdl.handle.net/20.500.12779/6141
Title: Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
Authors: Akselsen, O. W.
Odlo, K.
Cheng, J. J.
Maccari, Giorgio
Botta, Maurizio 
Hansen, T. V.
Keywords: Combretastatin A-1 Tubulin Angiogenesis 1; 2; 3-Triazoles Molecular modeling
Issue Date: 2012
Project: None 
Journal: BIOORGANIC & MEDICINAL CHEMISTRY
Abstract: 
The synthesis, cytotoxicity, inhibition of tubulin polymerization data and anti-angiogenetic effects of seven 1,5-disubstituted 1,2,3-triazole analogs and two 1,4-disubstituted 1,2,3-triazole analogs of combretastatin A-1 (1) are reported herein. The biological studies revealed that the 1,5-disubstituted 1,2,3-triazoles 3-methoxy-6-(1-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazol-5-yl)benzene-1,2-diol (6), 3-methoxy-6-(1-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazol-5-yl)benzene-1,2-diamine (8) and 5-(2,3-difluoro-4-methoxyphenyl)-1-(3,4,5-trimethoxyphenyl)-1H-1,2,3-triazole (9) were the three most active compounds regarding inhibition of both tubulin polymerization and angiogenesis. Molecular modeling studies revealed that combretastatins 1 and 2 and analogs 5-11 could be successfully docked into the colchicine binding site of α,β-tubulin.
Description: 
40470
URI: http://hdl.handle.net/20.500.12779/6141
ISSN: 1464-3391
DOI: 10.1016/j.bmc.2011.11.010
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