The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 1: Hydroxynaphthalene derivatives

Authors
Marsilje, TH Milkiewicz, KL Hangauer, DG
Citation
Th. Marsilje et al., The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 1: Hydroxynaphthalene derivatives, BIOORG MED, 10(5), 2000, pp. 477-481
Citations number
20
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
5
Year of publication
2000
Pages
477 - 481
Database
ISI
SICI code
0960-894X(20000306)10:5<477:TDSAAO>2.0.ZU;2-A
Abstract
A series of hydroxynaphthalene pp60(c-src) non-peptide inhibitors was desig ned, using the crystal structure of the insulin receptor tyrosine kinase as a qualitative model, to target the peptide substrate binding site. Represe ntative inhibitors were shown to bind non-competitively with respect to ATP . (C) 2000 Elsevier Science Ltd. All rights reserved.