Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity

…, S Kasibhatla, A Pervin, H Zhang, S Jiang…

Index: Kemnitzer, William; Drewe, John; Jiang, Songchun; Zhang, Hong; Crogan-Grundy, Candace; Labreque, Denis; Bubenick, Monica; Attardo, Giorgio; Denis, Real; Lamothe, Serge; Gourdeau, Henriette; Tseng, Ben; Kasibhatla, Shailaja; Sui, Xiong Cai Journal of Medicinal Chemistry, 2008 , vol. 51, # 3 p. 417 - 423

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Citation Number: 53

Abstract

Using a live cell, high-throughput caspase-3 activator assay, we have identified a novel series of 4-anilinoquinazolines as inducers of apoptosis. In this report, we discuss the discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine, compound 2b (EP128265, MPI-0441138) as a highly active inducer of apoptosis (EC50 for caspase activation of 2 nM) and as a potent inhibitor of cell proliferation (GI50 of 2 nM) in T47D ...