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 language||English (US)|
|Number of pages||6|
|State||Published - Jan 1 1995|
ASJC Scopus subject areas
- Pharmaceutical Science
- Drug Discovery