Effect of alteration of the heterocyclic nucleus of ILV on its isoform selectivity for PKC. Palladium catalyzed route to benzofuran analogues of ILV

A. P. Kozikowski, D. Ma, L. Du, N. E. Lewin, P. M. Blumberg

Research output: Contribution to journalArticlepeer-review

Abstract

A palladium catalyzed route for the preparation of several benzofuran analogues of the PKC activator indolactam V (ILV) is described together with the ability of these compounds to activate the isoforms of PKC. The benzofuran analogues of ILV are shown to activate PKC with a slightly different pattern of isotype selectivity than ILV or 7-n-octyl-ILV. Moreover, in an examination of the effect of stereochemistry at the C-14 center of the teleocidins on PKC binding activity, a clear preference for R-stereochemistry at the C-14 center was found, thus providing additional verification of previously published structural correlations between the families of PKC activators.

Original languageEnglish (US)
Pages (from-to)425-430
Number of pages6
JournalFarmaco
Volume50
Issue number6
StatePublished - Jan 1 1995

ASJC Scopus subject areas

  • Pharmaceutical Science
  • Drug Discovery

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