ChemInform Abstract: Synthesis and Protein Kinase C Inhibitory Activities of Acyclic Balanol Analogues That are Highly Selective for Protein Kinase C Over Protein Kinase A.

✍ Scribed by J. M. DEFAUW; M. M. MURPHY; G. E. JUN. JAGDMANN; H. HU; J. W. LAMPE; S. P. HOLLINSHEAD; T. J. MITCHELL; H. M. CRANE; J. M. HEERDING; J. S. MENDOZA; J. E. DAVIS; J. W. DARGES; F. R. HUBBARD; S. E. HALL

• Publisher: John Wiley and Sons
• Year: 2010
• Weight: 31 KB
• Volume: 28
• Category: Article
• ISSN: 0931-7597
• DOI: 10.1002/chin.199716274

✦ Synopsis

A series of analogues of balanol (I) in which the perhydroazepine ring and the p-hydroxybenzamide moiety have been combined into a simple acyclic linked unit are evaluated for their inhibitory properties. It is found that a three-carbon linkage is optimal. Substitution on the three-carbon chain is investigated and the most active analogues found are racemic and optically active (VIII) and its enantiomers. Reintroduction of a ring in form of an anti-substituted pyrrolidine and cyclopentane ring leads also to potent compounds. -(DEFAUW,