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
相关论文
共 16 条
[1]  
BIRD CW, 1984, COMPREHENSIVE HETE 3, V4
[2]  
Davis KJ, 1997, INDIAN J CHEM B, V36, P211
[3]  
Farina V., 1997, ORGANIC REACTIONS, V50
[4]  
FOURNARI P, 1967, B SOC CHIM FR, P4115
[5]   CONVENIENT SYNTHESIS OF VARIOUS TERHETEROCYCLIC COMPOUNDS BY PD(O)-CATALYZED COUPLING REACTIONS [J].
GRONOWITZ, S ;
PETERS, D .
HETEROCYCLES, 1990, 30 (01) :645-658
[6]   4,5-DISUBSTITUTION OF 3-THIOPHENE ALDEHYDE [J].
GRONOWITZ, S ;
ANDER, I .
TETRAHEDRON, 1976, 32 (12) :1403-1406
[7]   Signal transduction by protein kinase mammalian cells [J].
Kanashiro, CA ;
Khalil, RA .
CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY, 1998, 25 (12) :974-985
[8]   Novel protein kinase C inhibitors:: α-terthiophene derivatives [J].
Kim, DSHL ;
Ashendel, CL ;
Zhou, Q ;
Chang, CT ;
Lee, ES ;
Chang, CJ .
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1998, 8 (19) :2695-2698
[9]  
MISTUMORI T, 1995, J AM CHEM SOC, V117, P2467
[10]  
Mochly-Rosen D, 1998, ADV PHARMACOL, V44, P91, DOI 10.1016/S1054-3589(08)60126-X