Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanol

Analogs 2–5 of balanol (−)-1, a potent protein kinase C (PKC) inhibitor, were prepared in which the perhydroazepine N atom was replaced with O, S, or C. Compounds 2 and 3 are found to show enhanced isozyme selectivity, despite the general trend of these analogs being less potent PKC inhibitors relative to balanol.