SAR156497 an exquisitely selective inhibitor of aurora kinases

4^th European Chemistry Congress

May 11-13, 2017 Barcelona, Spain

Jean-Christophe Carry

Sanofi, France

Posters & Accepted Abstracts: Chem Sci J

Abstract :

The Aurora family of serine/threonine kinases is essential for mitosis. Their crucial role in cell cycle regulation and aberrant expression in a broad range of malignancies have been demonstrated and have prompted intensive search for small molecule Aurora inhibitors. Indeed, over ten of them have reached the clinic as potential anticancer therapies. We will report the discovery and optimization of a novel series of tricyclic molecules that has led to SAR156497, an exquisitely selective Aurora A, -B and -C inhibitor with in vitro and in vivo efficacy. We will also provide insights into its mode of binding to its target proteins from X-Ray data, which could explain its selectivity. jean-christophe.carry@sanofi.com