Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C

7-Methoxy-8-decynyl-benzolactam-V8 4 is synthesized using a catalytic asymmetric alkylation reaction as a key step. This compound shows potent activity to three PKC isozymes tested (Ki=45.6, 91.1, and 121.3 nM to PKCα, δ, and , respectively), indicating that introduction of a suitable substituent at the 7-position of 8-decynyl-benzolactam-V8 only slightly reduces the PKC binding affinity.