title: The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives.
abstract: 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.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, State University of New York at Buffalo, 14260-1200, USA.
authors.forename: K L
authors.initials: KL
authors.lastname: Milkiewicz
authors.forename: T H
authors.initials: TH
authors.lastname: Marsilje
authors.forename: R P
authors.initials: RP
authors.lastname: Woodworth
authors.forename: N
authors.initials: N
authors.lastname: Bifulco
authors.forename: M J
authors.initials: MJ
authors.lastname: Hangauer
authors.forename: D G
authors.initials: DG
authors.lastname: Hangauer
mesh_terms: 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*
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; D000255:Adenosine Triphosphate; D019061:src-Family Kinases