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Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety
- Source :
- Journal of medicinal chemistry. 40(2)
- 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 :
- biology
Chemistry
Kinase
Stereochemistry
medicine.drug_class
Molecular Conformation
Carboxamide
Azepines
Chemical synthesis
Balanol
Isoenzymes
chemistry.chemical_compound
Structure-Activity Relationship
Enzyme inhibitor
Drug Discovery
biology.protein
medicine
Hydroxybenzoates
Molecular Medicine
Moiety
Enzyme Inhibitors
Protein kinase A
Protein kinase C
Protein Kinase C
Subjects
Details
- ISSN :
- 00222623
- Volume :
- 40
- Issue :
- 2
- Database :
- OpenAIRE
- Journal :
- Journal of medicinal chemistry
- Accession number :
- edsair.doi.dedup.....21599790538203002f0f544fb11828bd