Novel protein kinase C inhibitors: alpha-terthiophene derivatives.
A series of alpha-terthiophene derivatives were prepared and their protein kinase C inhibitory activity were evaluated. The aldehyde derivatives were most potent inhibitors (IC50 < 1 microM). alpha-Terthiophene monoaldehyde was inactive in the inhibitions of protein kinase A, mitogen activated protein kinase and protein tyrosine kinase.
Kim
D S
DS
Department of Medicinal Chemistry, Purdue University, West Lafayette, IN 47907-1333, USA.
Ashendel
C L
CL
Zhou
Q
Q
Chang
C T
CT
Lee
E S
ES
Chang
C J
CJ
D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis* / Q000494:pharmacology*
D004791:Enzyme Inhibitors; D013876:Thiophenes; C019101:alpha-terthienyl; D011493:Protein Kinase C