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

J L Buchanan; C B Vu; T J Merry; E G Corpuz; S G Pradeepan; U N Mani; M Yang; H R Plake; V M Varkhedkar; B A Lynch; I A MacNeil; K A Loiacono; C L Tiong; D A Holt

doi:10.1016/s0960-894x(99)00389-3

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

Bioorg Med Chem Lett. 1999 Aug 16;9(16):2359-64. doi: 10.1016/s0960-894x(99)00389-3.

Authors

J L Buchanan¹, C B Vu, T J Merry, E G Corpuz, S G Pradeepan, U N Mani, M Yang, H R Plake, V M Varkhedkar, B A Lynch, I A MacNeil, K A Loiacono, C L Tiong, D A Holt

Affiliation

¹ ARIAD Pharmaceuticals, Inc., Cambridge, Massachusetts 02139-4234, USA. john.buchanan@ariad.com

PMID: 10476869
DOI: 10.1016/s0960-894x(99)00389-3

Abstract

The structure-activity relationships (SAR) of a novel class of Src SH2 inhibitors are described. Variation at the pY+1 and pY+3 side chain positions using 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-pYEEI-NH2.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Structure-Activity Relationship
Thiazoles / chemistry*
Thiazoles / pharmacology*
src Homology Domains*

Substances

Thiazoles