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.
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收藏
页码：327 / 345
页数：19
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