SYNTHESIS AND BIOLOGICAL-ACTIVITY OF NOVEL 3'-TRIFLUOROMETHYL TAXOIDS

Authors
OJIMA I SLATER JC PERA P VEITH JM ABOUABDELLAH A BEGUE JP BERNACKI RJ
Citation
I. Ojima et al., SYNTHESIS AND BIOLOGICAL-ACTIVITY OF NOVEL 3'-TRIFLUOROMETHYL TAXOIDS, Bioorganic & medicinal chemistry letters, 7(2), 1997, pp. 133-138
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
2
Year of publication
1997
Pages
133 - 138
Database
ISI
SICI code
0960-894X(1997)7:2<133:SABON3>2.0.ZU;2-V
Abstract
Second generation taxoids possessing a trifluoromethyl moiety in place of the 3'-phenyl group are synthesized by means of the beta-Lactam Sy nthon Method. The in vitro cytotoxicities of these new taxoids are eva luated against several different human cancer cell lines and found to exhibit greatly enhanced activities as compared to those of paclitaxel and docetaxel. The activity enhancement is most remarkable against a drug-resistant breast cancer cell line, MCF7-R, expressing MDR phenoty pe. (C) 1997, Elsevier Science Ltd.