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, 40 (2), 226-35

Synthesis and Protein Kinase C Inhibitory Activities of Balanol Analogs With Replacement of the Perhydroazepine Moiety

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Synthesis and Protein Kinase C Inhibitory Activities of Balanol Analogs With Replacement of the Perhydroazepine Moiety

Y S Lai et al. J Med Chem.

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.

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