title: Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase.
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.
authors.affiliation: Department of Chemistry, SUGEN, Inc., 230 East Grand Avenue, South San Francisco, CA 94080, USA.
authors.forename: Huiping
authors.initials: H
authors.lastname: Guan
authors.forename: A Douglas
authors.initials: AD
authors.lastname: Laird
authors.forename: Robert A
authors.initials: RA
authors.lastname: Blake
authors.forename: Cho
authors.initials: C
authors.lastname: Tang
authors.forename: Chris
authors.initials: C
authors.lastname: Liang
mesh_terms: D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D007211:Indoles; C456900:indolin-2-one; D019061:src-Family Kinases