Novel protein kinase C inhibitors: synthesis and PKC inhibition of β-substituted polythiophene derivatives

A series of β-substituted polythiophene derivatives was synthesized through palladium-catalyzed coupling reaction. Their structure-protein kinase C (PKC) inhibitory activity relationship was studied. The carboxaldehyde and hydroxymethyl derivatives of α-terthiophene were potent PKC inhibitors (IC50 = 10−7 M).