The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 1: hydroxynaphthalene derivatives.
A series of hydroxynaphthalene pp60(c-src) non-peptide inhibitors was designed, using the crystal structure of the insulin receptor tyrosine kinase as a qualitative model, to target the peptide substrate binding site. Representative inhibitors were shown to bind non-competitively with respect to ATP.
Marsilje
T H
TH
Department of Medicinal Chemistry, School of Pharmacy, State University of New York at Buffalo, 14260-1200, USA.
Milkiewicz
K L
KL
Hangauer
D G
DG
D000255:Adenosine Triphosphate / Q000378:metabolism*; D001667:Binding, Competitive; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D008958:Models, Molecular; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D009281:Naphthalenes; D000255:Adenosine Triphosphate; D019061:src-Family Kinases