2. Academic Validation
  3. SAR156497, an exquisitely selective inhibitor of aurora kinases

SAR156497, an exquisitely selective inhibitor of aurora kinases

  • J Med Chem. 2015 Jan 8;58(1):362-75. doi: 10.1021/jm501326k.
Jean-Christophe Carry 1,  François Clerc,  Hervé Minoux,  Laurent Schio,  Jacques Mauger,  Anil Nair,  Eric Parmantier,  Ronan Le Moigne,  Cécile Delorme,  Jean-Paul Nicolas,  Alain Krick,  Pierre-Yves Abécassis,  Véronique Crocq-Stuerga,  Stéphanie Pouzieux,  Laure Delarbre,  Sébastien Maignan,  Thomas Bertrand,  Kirsten Bjergarde,  Nina Ma,  Sylvette Lachaud,  Houlfa Guizani,  Rémi Lebel,  Gilles Doerflinger,  Sylvie Monget,  Sébastien Perron,  Francis Gasse,  Odile Angouillant-Boniface,  Bruno Filoche-Rommé,  Michel Murer,  Sylvie Gontier,  Céline Prévost,  Marie-Line Monteiro,  Cécile Combeau
Affiliations

Affiliation

  • 1 Oncology Drug Discovery, ‡Structure Design Informatics, §Disposition Safety Animal Research, ∥Chemical Development, and ⊥Analytical Sciences, Sanofi , 13 Quai Jules Guesde, 94403 Vitry-sur-Seine, France.
PMID: 25369539 DOI: 10.1021/jm501326k
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 10 of them have reached the clinic as potential Anticancer therapies. We report herein 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 also provide insights into its mode of binding to its target proteins, which could explain its selectivity.

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