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

…, T Zhang, G Wang, AP Kozikowski, NE Lewin…

文献索引：Ma, Dawei; Zhang, Tao; Wang, Guoqiang; Kozikowski, Alan P.; Lewin, Nancy E.; Blumberg, Peter M. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 2 p. 99 - 101

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被引用次数: 19

摘要

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 ε, respectively), indicating that introduction of a suitable substituent at the 7-position of 8-decynyl-benzolactam-V8 only slightly reduces the PKC binding affinity.