Synthesis and biological evaluation of paclitaxel-thiocolchicine hybrids.

作者信息

Danieli Bruno, Giardini Alessandra, Lesma Giordano, Passarella Daniele, Silvani Alessandra, Appendino Giovanni, Noncovich Alain, Fontana Gabriele, Bombardelli Ezio, Sterner Olov

机构信息

Dipartimento di Chimica Organica e Industriale, Università degli Studi di Milano, Via Venezian 21, I-20133 Milano.

出版信息

Chem Biodivers. 2004 Feb;1(2):327-45. doi: 10.1002/cbdv.200490029.

DOI:10.1002/cbdv.200490029

PMID:17191851

Abstract

The bifunctional taxoid-colchicinoid hybrids 6-8 were synthesized and evaluated in assays of cytotoxicity and tubulin assembly/disassembly. All compounds showed a high degree of cytotoxicity, but, while 6 and 7 behaved as bifunctional tubulin binders not unlike an equimolecular mixture of taxol and thiocolchicine, 8 was surprisingly devoid of tubulin activity, acting on a distinct and yet to identify molecular target.

摘要