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  • Synthesis and biological evaluation of paclitaxel-thiocolchicine hybrids.

Synthesis and biological evaluation of paclitaxel-thiocolchicine hybrids.

Chemistry & biodiversity (2006-12-29)
Bruno Danieli, Alessandra Giardini, Giordano Lesma, Daniele Passarella, Alessandra Silvani, Giovanni Appendino, Alain Noncovich, Gabriele Fontana, Ezio Bombardelli, Olov Sterner
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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Thiocolchicine, ≥97% (HPLC)