PROTEIN-KINASE-C INHIBITORY ACTIVITIES OF BALANOL ANALOGS BEARING CARBOXYLIC-ACID REPLACEMENTS

Authors
HEERDING JM LAMPE JW DARGES JW STAMPER ML
Citation
Jm. Heerding et al., PROTEIN-KINASE-C INHIBITORY ACTIVITIES OF BALANOL ANALOGS BEARING CARBOXYLIC-ACID REPLACEMENTS, Bioorganic & medicinal chemistry letters, 5(16), 1995, pp. 1839-1842
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
16
Year of publication
1995
Pages
1839 - 1842
Database
ISI
SICI code
0960-894X(1995)5:16<1839:PIAOBA>2.0.ZU;2-8
Abstract
A variety of balanol analogs bearing carboxylic acid replacements (ami des, sulfonamides and tetrazoles) were synthesized and evaluated for p rotein kinase C (PKC) inhibitory activity. In general, those compounds which bear an acidic proton (pKa less than or equal to 7.6) display p otent PKC activity, and show selectivity for PKC over other kinases. P rodrugs are excellent tools for increasing cellular activity of some a cid replacements.