Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase

Huiping Guan; A Douglas Laird; Robert A Blake; Cho Tang; Chris Liang

doi:10.1016/j.bmcl.2003.09.069

Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase

Bioorg Med Chem Lett. 2004 Jan 5;14(1):187-90. doi: 10.1016/j.bmcl.2003.09.069.

Authors

Huiping Guan¹, A Douglas Laird, Robert A Blake, Cho Tang, Chris Liang

Affiliation

¹ Department of Chemistry, SUGEN, Inc., 230 East Grand Avenue, South San Francisco, CA 94080, USA.

PMID: 14684325
DOI: 10.1016/j.bmcl.2003.09.069

Abstract

A novel series of substituted 3-[3-(aminopropyl)-4,5,6,7-tetrahydro-1H-indol-2-ylmethylene]-1,3-dihydro-indole-2-ones was discovered as potent inhibitors of the non-receptor tyrosine kinase Src and Yes. A structure-activity relationship was developed in order to optimize their potency and selectivity. Syntheses of these compounds are also described herein.

MeSH terms

Drug Design
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Indoles / chemical synthesis*
Indoles / pharmacology*
Structure-Activity Relationship
src-Family Kinases / antagonists & inhibitors*
src-Family Kinases / metabolism

Substances

Enzyme Inhibitors
Indoles
indolin-2-one
src-Family Kinases