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 …
LJ Lombardo, FY Lee, P Chen, D Norris… - Journal of medicinal …, 2004 - ACS Publications
LJ Lombardo, FY Lee, P Chen, D Norris, JC Barrish, K Behnia, S Castaneda, LAM Cornelius…
Journal of medicinal chemistry, 2004•ACS PublicationsA 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 myelogenous leukemia (CML), demonstrating complete tumor
regressions and low toxicity at multiple dose levels. On the basis of its robust in vivo activity
and favorable pharmacokinetic profile, 13 was selected for additional characterization for …
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 myelogenous leukemia (CML), demonstrating complete tumor
regressions and low toxicity at multiple dose levels. On the basis of its robust in vivo activity
and favorable pharmacokinetic profile, 13 was selected for additional characterization for …
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 myelogenous leukemia (CML), demonstrating complete tumor regressions and low toxicity at multiple dose levels. On the basis of its robust in vivo activity and favorable pharmacokinetic profile, 13 was selected for additional characterization for oncology indications.
ACS Publications