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Protein kinase C inhibitory activities of balanol analogs bearing carboxylic acid replacements

✍ Scribed by Julia M. Heerding; John W. Lampe; James W. Darges; Mark L. Stamper

Book ID: 103983027
Publisher: Elsevier Science
Year: 1995
Tongue: English
Weight: 255 KB
Volume: 5
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(95)00303-b

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✦ Synopsis

A variety of balanol analogs bearing carboxylic acid replacements (amides, sulfonamides and tetrazoles) were synthesized and evaluated for protein kinase C (PKC) inhibitory activity. In general, those compounds which bear an acidic proton (pKa < 7.6) display potent PKC activity, and show selectivity for PKC over other kinases. Prodrugs are excellent tools for increasing cellular activity of some acid replacements.

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