HALOHYDRIN ANALOGS OF CRYPTOPHYCIN 1 - SYNTHESIS AND BIOLOGICAL-ACTIVITY

Authors
GEORG GI ALI SM STELLA VJ WAUGH WN HIMES RH
Citation
Gi. Georg et al., HALOHYDRIN ANALOGS OF CRYPTOPHYCIN 1 - SYNTHESIS AND BIOLOGICAL-ACTIVITY, Bioorganic & medicinal chemistry letters, 8(15), 1998, pp. 1959-1962
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
8
Issue
15
Year of publication
1998
Pages
1959 - 1962
Database
ISI
SICI code
0960-894X(1998)8:15<1959:HAOC1->2.0.ZU;2-L
Abstract
The chloro-, bromo-, and iodo-derivatives 2-4 of the antimitotic drug cryptophycin 1 were synthesized by opening the epoxide ring. The biolo gical activities of the compounds were tested in an in vitro microtubu le assembly and a cell proliferation assay. The chloro-derivative 2 sh owed lower activity in the tubulin assay compared to 3 and 4, but they all showed similar inhibition in the proliferation assay. (C) 1998 El sevier Science Ltd. All rights reserved.