Synthesis and Modeling Study of
(2S,5R,6R)- and (2S,5R,6S)-6-Hydroxy-
8-(1-decynyl)-benzolactam-V8 as Protein
Kinase C Modulators

Wei, Zhi-Liang; Sakamuri, Sukumar; Petukhov, Pavel A.; George, Clifford; Lewin, Nancy E.; Blumberg, Peter M.; Kozikowski, Alan P.

doi:10.1021/ol026013u.s001

Synthesis and Modeling Study of (2S,5R,6R)- and (2S,5R,6S)-6-Hydroxy- 8-(1-decynyl)-benzolactam-V8 as Protein Kinase C Modulators

https://doi.org/10.1021/ol026013u.s001
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journal contribution

posted on 2002-06-04, 00:00 authored by Zhi-Liang Wei, Sukumar Sakamuri, Pavel A. Petukhov, Clifford George, Nancy E. Lewin, Peter M. Blumberg, Alan P. Kozikowski

Both (2S,5R,6R)- and (2S,5R,6S)-6-hydroxy-8-(1-decynyl)benzolactam-V8 were designed and synthesized as PKC modulators. Biological assays reveal the (6R)-ligand to be 20-fold more potent than its (6S)-counterpart in binding to PKCα.