The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives.
As part of a continuing effort to identify novel scaffolds that inhibit the pp60(c-src) protein tyrosine kinase, a series of hydroxyindole amides was rationally designed and synthesized. The most potent derivative was found to bind non-competitively with respect to ATP.
Milkiewicz
K L
KL
Department of Medicinal Chemistry, School of Pharmacy, State University of New York at Buffalo, 14260-1200, USA.
Marsilje
T H
TH
Woodworth
R P
RP
Bifulco
N
N
Hangauer
M J
MJ
Hangauer
D G
DG
D000255:Adenosine Triphosphate / Q000378:metabolism*; D001667:Binding, Competitive / Q000187:drug effects; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008958:Models, Molecular; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D007211:Indoles; D000255:Adenosine Triphosphate; D019061:src-Family Kinases