Synthesis and biological evaluation of fluorescently labeled epothilone analogs for tubulin binding studies
Synthesis and biological evaluation of fluorescently labeled epothilone analogs for tubulin binding studies
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DOI：
10.1016/j.tet.2003.10.024
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发表时间：
2003-12-08
期刊：
影响因子：
2.1
通讯作者：
Kingston, DGI
中科院分区：
文献类型：
--
作者：
Ganesh, T;Schilling, JK;Kingston, DGI
两个荧光标记的埃坡霉素14和15已被合成使用Nicolaou的macrolactonization和Stille耦合策略的修改。化合物对A2870卵巢癌细胞系的细胞毒性分别为6.1和2.7 μ g/mL，对PC-3前列腺癌细胞系的细胞毒性分别为0.5和1.0 μ g/mL。微管蛋白的临界浓度分别为0.5和1.0 μ M的存在下，14和15，相比之下，0.3 μ M的紫杉醇。描述了这两种分子在溶液中和与微管结合的荧光性质。(C)2003 Elsevier Ltd.保留所有权利。
The two fluorescently labeled epothilones 14 and 15 have been synthesized using a modification of Nicolaou's macrolactonization and Stille coupling strategy. The cytotoxicities of the compounds were 6.1 and 2.7 mug/mL, respectively, against the A2870 ovarian cancer cell line, and 0.5 and 1.0 mug/mL, respectively, against the PC-3 prostate cancer cell line. The critical concentration of tubulin was 0.5 and 1.0 muM in the presence of 14 and 15, respectively, compared with 0.3 muM for paclitaxel. The fluorescent properties of the two molecules in solution and bound to microtubules are described. (C) 2003 Elsevier Ltd. All rights reserved.