Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation

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

Index: Suarez, Rosa M.; Chevot, Franciane; Cavagnino, Andrea; Saettel, Nicolas; Radvanyi, Francois; Piguel, Sandrine; Bernard-Pierrot, Isabelle; Stoven, Veronique; Legraverend, Michel European Journal of Medicinal Chemistry, 2013 , vol. 61, p. 2 - 25

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Citation Number: 13

Abstract

The TAM subfamily of Receptor Tyrosine Kinases (RTKs) contains three human proteins of therapeutical interest, Axl, Mer, and Tyro3. Our goal was to design a type II inhibitor specific for this family, ie able to interact with the allosteric pocket and with the hinge region of the kinase. We report the synthesis of several series of purine analogues of BMS-777607. The structural diversity of the designed inhibitors was expected to modify the interactions ...