Structure-activity relationships of a novel class of Src SH2 inhibitors

Authors
Buchanan, JL Vu, CB Merry, TJ Corpuz, EG Pradeepan, SG Mani, UN Yang, M Plake, HR Varkhedkar, VM Lynch, BA MacNeil, IA Loiacono, KA Tiong, CL Holt, DA
Citation
Jl. Buchanan et al., Structure-activity relationships of a novel class of Src SH2 inhibitors, BIOORG MED, 9(16), 1999, pp. 2359-2364
Citations number
19
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
16
Year of publication
1999
Pages
2359 - 2364
Database
ISI
SICI code
0960-894X(19990816)9:16<2359:SROANC>2.0.ZU;2-X
Abstract
The structure-activity relationships (SAR) of a novel class of Src SH2 inhi bitors are described. Variation at the pY+1 and pY+3 side chain positions u sing 2,4- and 2,5-substituted thiazoles and 1,2,4-oxadiazoles as scaffolds resulted in inhibitors that bound as well as the standard tetrapeptide Ac-p YEEI-NH2. (C) 1999 Elsevier Science Ltd. All rights reserved.