Synthesis and microtubule binding of fluorescent paclitaxel derivatives

被引:14
作者
Baloglu, E
Kingston, DGI
Patel, P
Chatterjee, SK
Bane, SL [1 ]
机构
[1] SUNY Binghamton, Dept Chem, Binghamton, NY 13902 USA
[2] Virginia Polytech Inst & State Univ, Dept Chem, Blacksburg, VA 24061 USA
关键词
D O I
10.1016/S0960-894X(01)00453-X
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The preparation of two new fluorescent derivatives of paclitaxel in which the fluorophore is bonded to paclitaxel at the C-10 position is reported, Both analogues, 10-deacetyl-10-(m-aminobenzoyl)paclitaxel (1, BTax) and 10-dcacetyl-10-[7-(diethylamino) coumarin-3-carbonyl]paclitaxel (2, CTax) retain good activity as promoters of in vitro tubulin assembly. Microtubule binding enhances the emission intensity of both probes. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2249 / 2252
页数:4
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