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

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

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

J Med Chem. 1997 Jan 17;40(2):226-35.

PubMed ID

9003521 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Balanol	cAMP-dependent protein kinase catalytic subunit alpha	IC 50 (nM)	50	N/A	N/A	Details
Balanol	cAMP-dependent protein kinase catalytic subunit alpha	IC 50 (nM)	5200	N/A	N/A	Details