New aminopyrimidine derivatives as inhibitors of the TAM family

…, I Bernard-Pierrot, V Stoven, M Legraverend

Index: Traore, Tenin; Cavagnino, Andrea; Saettel, Nicolas; Radvanyi, Francois; Piguel, Sandrine; Bernard-Pierrot, Isabelle; Stoven, Veronique; Legraverend, Michel European Journal of Medicinal Chemistry, 2013 , vol. 70, p. 789 - 801

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Citation Number: 3

Abstract

Abstract In this study, we describe the synthesis of new pyrimidine analogs of BMS-777607, a potent and selective inhibitor of Met kinase. Inhibition of Met and Axl remained high whereas inhibition of Tyro3 and Mer decreased to some extend. The preferential moderate inhibition of the non-phosphorylated form of Abl1 of some derivatives suggests that they behave as type II inhibitors. This hypothesis was confirmed by docking studies into the ...