Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives.
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).
Xu
W C
WC
Department of Medicinal Chemistry, School of Pharmacy, Purdue University, West Lafayette, IN 47907-1333, USA.
Zhou
Q
Q
Ashendel
C L
CL
Chang
C T
CT
Chang
C J
CJ
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011108:Polymers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D004791:Enzyme Inhibitors; D011108:Polymers; D013876:Thiophenes; C019101:alpha-terthienyl; C066730:polythiophene; D011493:Protein Kinase C