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.
Original language | English (US) |
---|---|
Pages (from-to) | 1959-1962 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 8 |
Issue number | 15 |
DOIs | |
State | Published - Aug 4 1998 |
Bibliographical note
Funding Information: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.