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

被引:26
|
作者
Xu, WC
Zhou, Q
Ashendel, CL
Chang, CT
Chang, CJ [1 ]
机构
[1] Purdue Univ, Sch Pharm, Dept Med Chem & Mol Pharmacol, W Lafayette, IN 47907 USA
[2] Union Chem Labs, Hsinchu, Taiwan
关键词
D O I
10.1016/S0960-894X(99)00375-3
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of beta-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 alpha-terthiophene were potent PKC inhibitors (IC50 = 10(-7) M). (C) 1999 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2279 / 2282
页数:4
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