4^th European Chemistry Congress

Biography

Biography: Jean-Christophe Carry

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.