SYNTHESIS AND PROTEIN-KINASE-C INHIBITORY ACTIVITIES OF INDANE ANALOGS OF BALANOL

Authors
HU H HOLLINSHEAD SP HALL SE KALTER K BALLAS LM
Citation
H. Hu et al., SYNTHESIS AND PROTEIN-KINASE-C INHIBITORY ACTIVITIES OF INDANE ANALOGS OF BALANOL, Bioorganic & medicinal chemistry letters, 6(8), 1996, pp. 973-978
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
8
Year of publication
1996
Pages
973 - 978
Database
ISI
SICI code
0960-894X(1996)6:8<973:SAPIAO>2.0.ZU;2-Z
Abstract
Regio- and stereoisomeric indane analogs (4-6) of balanol (-)-1, a pot ent protein kinase C (PKC) inhibitor, were synthesized in which the pe rhydroazepine of balanol was replaced by an indane nucleus. Analog (-) -4 and its racemic regioisomer 6 were found to have highly potent PKC inhibitory activities. In addition, compound (-)-4 displayed excellent kinase selectivity for PKC over PKA. Copyright (C) 1996 Elsevier Scie nce Ltd