The chloro-, bromo-, and iodo-derivatives 2-4 of the antimitotic drug cryptophycin 1 were synthesized by opening the epoxide ring. The biological activities of the compounds were tested in an in vitro microtubule assembly and a cell proliferation assay. The chloro-derivative 2 showed lower activity in the tubulin assay compared to 3 and 4, but they all showed similar inhibition in the proliferation assay.
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Acknowledgments. These studies were supported by NIH research grant CA70369. S. M. Ali was a recipient of a postdoctoral scholar grant from the Kansas Health Foundation. Cryptophycin 1 was kindly supplied by R. E. Schwartz, Merck, Sharp & Dohme Research Laboratories.