Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 16, Issue 9, Pages 4829-4838Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2008.03.049
Keywords
combretastatin A-4; cytotoxic; 1,2,3-triazoles; molecular modeling
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A series of cis-restricted 1,5-disubstituted 1,2,3-triazole analogues of combretastatin A-4 (1) have been prepared. The triazole 12f, 2-methoxy-5-(1-(3,4,5- trimethoxyphenyl)-1H-1,2,3-triazol-5-yl) aniline, displayed potent cytotoxic activity against several cancer cell lines with IC50 values in the nanomolar range. The ability of triazoles to inhibit tubulin polymerization has been evaluated, and 12f inhibited tubulin polymerization with IC50 = 4.8 mu M. Molecular modeling experiments involving 12f and the colchicine binding site of alpha,beta-tubulin showed that the triazole moiety interacts with beta-tubulin via hydrogen bonding with several amino acids. (c) 2008 Elsevier Ltd. All rights reserved.
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