RING SIZE EFFECT IN THE PKC INHIBITORY ACTIVITIES OF PERHYDROAZEPINE ANALOGS OF BALANOL

被引:28
作者
LAI, YS
MENALDINO, DS
NICHOLS, JB
JAGDMANN, GE
MYLOTT, F
GILLESPIE, J
HALL, SE
机构
[1] Sphinx Pharmaceuticals A Division of Eli Lilly and Company, Durham, NC 27707
关键词
D O I
10.1016/0960-894X(95)00365-Z
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Analogs 3-5 of balanol (-)-1, a potent protein kinase C (PKC) inhibitor, were synthesized with the perhydroazepine moiety replaced by a smaller ring. Their in vitro inhibitory activities against PKC revealed a significant relationship between ring size and potency.
引用
收藏
页码:2151 / 2154
页数:4
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