HETEROATOM EFFECT IN THE PKC INHIBITORY ACTIVITIES OF PERHYDROAZEPINEANALOGS OF BALANOL

Authors
LAI YS STAMPER M
Citation
Ys. Lai et M. Stamper, HETEROATOM EFFECT IN THE PKC INHIBITORY ACTIVITIES OF PERHYDROAZEPINEANALOGS OF BALANOL, Bioorganic & medicinal chemistry letters, 5(18), 1995, pp. 2147-2150
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
18
Year of publication
1995
Pages
2147 - 2150
Database
ISI
SICI code
0960-894X(1995)5:18<2147:HEITPI>2.0.ZU;2-1
Abstract
Analogs 2-5 of balanol (-)-1, a potent protein kinase C (PKC) inhibito r, were prepared in which the perhydroazepine N atom was replaced with O, S, or C. Compounds 2 and 3 are found to show enhanced isozyme sele ctivity, despite the general trend of these analogs being less potent PKC inhibitors relative to balanol.