Document Report Card

ID: ALA1130164

Journal: J Med Chem

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

Authors: Lai YS, Mendoza JS, Jagdmann GE, Menaldino DS, Biggers CK, Heerding JM, Wilson JW, Hall SE, Jiang JB, Janzen WP, Ballas LM.

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.

CiteXplore: 9003521

DOI: 10.1021/jm960497g