BINDING SELECTIVITY OF 1-OR 12-SUBSTITUTED INDOLACTAM DERIVATIVES FOR PROTEIN KINASE C ISOZYMES

摘要

The selectivity with which 1- or 12-substituted analogues of indolactam-V (1) bind protein kinase C (PKC) isozymes was examined.Moderate selectivity for novel PKC isozymes over conventional PKC isozymes was observed in the case of indolactam-nV (13) and indolactam-L (14) without an a-branched side chain at position 12.The introduction of a bulky isopropyl group to position 1 of 1 drastically increased the selectivity for novel PKC isozymes.