Abstract
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 μg/mL, respectively, against the A2870 ovarian cancer cell line, and 0.5 and 1.0 μg/mL, respectively, against the PC-3 prostate cancer cell line. The critical concentration of tubulin was 0.5 and 1.0 μM in the presence of 14 and 15 , respectively, compared with 0.3 μM for paclitaxel. The fluorescent properties of the two molecules in solution and bound to microtubules are described.
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