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]
- 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