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Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety

Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety

Authors :
William P. Janzen
Wilson Jw
J. S. Mendoza
Steven E. Hall
Lawrence M. Ballas
Jagdmann Ge
Biggers Ck
David S. Menaldino
Heerding Jm
Jack B. Jiang
Yen-Shi Lai
Source :
Journal of medicinal chemistry. 40(2)
Publication Year :
1997

Abstract

Balanol is a potent protein kinase C (PKC) inhibitor that is structurally composed of a benzophenone diacid, a 4-hydroxybenzamide, and a perhydroazepine ring. A number of balanol analogs in which the perhydroazepine moiety is replaced have been synthesized and their biological activities evaluated against both PKC and cAMP-dependent kinase (PKA). The results suggested that the activity and the isozyme/kinase selectivity of these compounds are largely related to the conformation about this nonaromatic structural element of the molecules.

Details

ISSN :
00222623
Volume :
40
Issue :
2
Database :
OpenAIRE
Journal :
Journal of medicinal chemistry
Accession number :
edsair.doi.dedup.....21599790538203002f0f544fb11828bd