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

WC Xu, Q Zhou, CL Ashendel, C Chang

文献索引：Xu, Wei-Chu; Zhou, Qin; Ashendel, Curtis L.; Chang, Ching-Te; Chang, Ching-Jer Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 15 p. 2279 - 2282

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被引用次数: 26

摘要

A series of β-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 α- terthiophene were potent PKC inhibitors (IC50= 10− 7 M).