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Halohydrin analogues of cryptophycin 1: synthesis and biological activity
G I Georg1, S M Ali, V J Stella
1Department of Medicinal Chemistry, University of Kansas, Lawrence 66045, USA.
Bioorganic & Medicinal Chemistry Letters
|January 5, 1999
Abstract:
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.