Back to Search
Start Over
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 1997 Jan 17; Vol. 40 (2), pp. 226-35. - 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.
- Subjects :
- Molecular Conformation
Structure-Activity Relationship
Azepines chemical synthesis
Azepines pharmacology
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Hydroxybenzoates chemical synthesis
Hydroxybenzoates pharmacology
Isoenzymes antagonists & inhibitors
Protein Kinase C antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 40
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 9003521
- Full Text :
- https://doi.org/10.1021/jm960497g