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

…, AD Laird, RA Blake, C Tang, C Liang

Index: Guan, Huiping; Laird, A. Douglas; Blake, Robert A.; Tang, Cho; Liang, Chris Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 1 p. 187 - 190

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Citation Number: 43

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.