Synthesis and biological evaluation of paclitaxel-thiocoichicine hybrids

被引：23

作者：

Danieli, B

Giardini, A

Lesma, G

Passarella, D

Silvani, A

Appendino, G

Noncovich, A

Fontana, G

Bombardelli, E

Sterner, O

机构：

[1] Univ Milan, Dipartimento Chim Organ & Ind, I-20133 Milan, Italy

[2] Univ Piemonte Orientale, Dipartimento Sci Chim Alimentari Farmaceut & Farm, I-28100 Novara, Italy

[3] Indena SPA, I-20139 Milan, Italy

[4] Lund Univ, Dept Bioorgan Chem, S Lund, Sweden

来源：

CHEMISTRY & BIODIVERSITY | 2004年 / 1卷 / 02期

关键词：

D O I：

10.1002/cbdv.200490029

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：327 / 345

页数：19

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