Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

LJ, Lombardo; FY, Lee; P, Chen; D, Norris; JC, Barrish; K, Behnia; S, Castaneda; LA, Cornelius; J, Das; AM, Doweyko; C, Fairchild; JT, Hunt; I, Inigo; K, Johnston; A, Kamath; D, Kan; H, Klei; P, Marathe; S, Pang; R, Peterson; S, Pitt; GL, Schieven; RJ, Schmidt; J, Tokarski; ML, Wen; J, Wityak; RM, Borzilleri

doi:10.1021/jm049486a

Public

Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

Shared by NobleBlocks on Dec 1, 2004 • 12:00 AM UTC

Authors:

Lombardo LJ

Lee FY

Chen P

Abstract

A series of substituted 2-(aminopyridyl)- and 2-(aminopyrimidinyl)thiazole-5-carboxamides was identified as potent Src/Abl kinase inhibitors with excellent antiproliferative activity against hematological and solid tumor cell lines. Compound 13 was orally active in a K562 xenograft model of chronic ...

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