EFFECT OF ALTERATION OF THE HETEROCYCLIC NUCLEUS OF ILV ON ITS ISOFORM SELECTIVITY FOR PKC - PALLADIUM-CATALYZED ROUTE TO BENZOFURAN ANALOGS OF ILV

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