Regio- and stereoisomeric indane analogs (4-6) of balanol (-)-1, a potent protein kinase C (PKC) inhibitor, were synthesized in which the perhydroazepine of balanol was replaced by an indane nucleus. Analog (-)-4 and its racemic regioisomer 6 were found to have highly potent PKC inhibitory activities. In addition, compound (-)-4 displayed excellent kinase selectivity for PKC over PKA.