SYNTHESIS AND ACTIVITY OF STAUROSPORINE ANALOGS WITH A LACTONE FUNCTIONALITY

Authors
YAMADA R FUKUDA K KAWANISHI M OHMORI Y NASU M SETO M SASAKI Y SUNAZUKA T ZHUORONG L FUNATO N IGUCHI M HARIGAYA Y IWAI Y OMURA S
Citation
R. Yamada et al., SYNTHESIS AND ACTIVITY OF STAUROSPORINE ANALOGS WITH A LACTONE FUNCTIONALITY, Bioorganic & medicinal chemistry letters, 6(16), 1996, pp. 1893-1896
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
16
Year of publication
1996
Pages
1893 - 1896
Database
ISI
SICI code
0960-894X(1996)6:16<1893:SAAOSA>2.0.ZU;2-Z
Abstract
Staurosporine analogs, whose gamma-lactam functionality was converted into gamma-lactone, were synthesized. The key step involves remarkably efficient ring-opening and then intramolecular cyclization reactions. In general, those compounds display potent anti-platelet aggregation activity and show higher selectivity against platelet as compared with smooth muscle contraction. Copyright (C) 1996 Elsevier Science Ltd