Synthesis and biological evaluation of B-ring modified colchicine and isocolchicine analogs

Bioorg Med Chem Lett. 2006 May 15;16(10):2761-4. doi: 10.1016/j.bmcl.2006.02.010.

Michael Cifuentes ¹, Brett Schilling, Rudravajhala Ravindra, Jacquelyn Winter, Mark E Janik

Affiliations

Affiliation

1 Department of Chemistry, SUNY Fredonia, Fredonia, NY 14063, USA.

PMID: 16504507 DOI: 10.1016/j.bmcl.2006.02.010

Abstract

A series of modified colchicine and isocolchicine analogs (C-7 substituent) were synthesized and evaluated in vitro against a PC3 Cancer cell line and for inhibition of microtubule polymerization. The colchicine analogs all displayed strong inhibition of tubulin polymerization, while compounds 6 and 20 also possessed an increased cytotoxic activity as compared to colchicine. More importantly, isocolchicine analogs 7, 15, and 17 showed inhibition of microtubule polymerization with IC(50) values ranging from 58 to 68muM. In addition, 7 displayed strong cytotoxic activity with an IC(50)=93nM which was more potent than colchicine analog 12.

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