Luc Bertin
Aventis Pharma
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Publication
Featured researches published by Luc Bertin.
Journal of Medicinal Chemistry | 2014
Victor Certal; Jean Christophe Carry; Frank Halley; Angela Virone-Oddos; Fabienne Thompson; Bruno Filoche-Romme; Youssef El-Ahmad; Andreas Karlsson; Véronique Charrier; Cécile Delorme; Alexey Rak; Pierre Yves Abecassis; Céline Amara; Loic Vincent; Hélène Bonnevaux; Jean Paul Nicolas; Magali Mathieu; Thomas Bertrand; Jean Pierre Marquette; Nadine Michot; Tsiala Benard; Marc Antoine Perrin; Olivier Lemaitre; Stéphane Guerif; Sébastien Perron; Sylvie Monget; Florence Gruss-Leleu; Gilles Doerflinger; Houlfa Guizani; Maurice Brollo
Compelling molecular biology publications have reported the implication of phosphoinositide kinase PI3Kβ in PTEN-deficient cell line growth and proliferation. These findings supported a scientific rationale for the development of PI3Kβ-specific inhibitors for the treatment of PTEN-deficient cancers. This paper describes the discovery of 2-[2-(2,3-dihydro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one (7) and the optimization of this new series of active and selective pyrimidone indoline amide PI3Kβ inhibitors. 2-[2-(2-Methyl-2,3-dihydro-indol-1-yl)-2-oxo-ethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one (28), identified following a carefully designed methyl scan, displayed improved physicochemical and in vitro pharmacokinetic properties. Structural biology efforts enabled the acquisition of the first X-ray cocrystal structure of p110β with the selective inhibitor compound 28 bound to the ATP site. The nonplanar binding mode described herein is consistent with observed structure-activity relationship for the series. Compound 28 demonstrated significant in vivo activity in a UACC-62 xenograft model in mice, warranting further preclinical investigation. Following successful development, compound 28 entered phase I/Ib clinical trial in patients with advanced cancer.
Bioorganic & Medicinal Chemistry Letters | 2014
Victor Certal; Frank Halley; Angela Virone-Oddos; Bruno Filoche-Romme; Jean Christophe Carry; Florence Gruss-Leleu; Luc Bertin; Houlfa Guizani; Fabienne Pilorge; Patrick Richepin; Andreas Karlsson; Véronique Charrier; Pierre Yves Abecassis; Loic Vincent; Jean Paul Nicolas; Christoph Lengauer; Carlos Garcia-Echeverria; Laurent Schio
In our continuous efforts to identify and develop novel targeted cancer treatments, a new morpholino-thiazole scaffold active against PI3Kβ has been identified. This Letter reports the optimization of this compound class to develop PI3Kβ isoform-selective inhibitors with suitable pharmacological properties.
Journal of Medicinal Chemistry | 2011
Francois Vallee; Chantal Carrez; Fabienne Pilorge; Alain Dupuy; Annick Parent; Luc Bertin; Fabienne Thompson; Paul Ferrari; Florence Fassy; Annabelle Lamberton; Anne Thomas; Rosalia Arrebola; Stéphane Guerif; Alexandre Rohaut; Victor Certal; Jean-Marie Ruxer; Cécile Delorme; Alain Jouanen; Jacques Dumas; Claudine Grépin; Cécile Combeau; Hélène Goulaouic; Norbert Dereu; Vincent Mikol; Patrick Mailliet; Hervé Minoux
Archive | 2006
Patrick Mailliet; Luc Bertin; Fabienne Thompson; Jean-Marie Ruxer; Fabienne Pilorge; Didier Benard; Hervé Minoux; Chantal Carrez; Hélène Goulaouic; Thierry Gouyon
Archive | 2010
Jean-Marie Ruxer; Victor Certal; Marcel Alasia; Luc Bertin; Hervé Minoux; Patrick Mailliet; Frank Halley; Maria Mendez-Perez
Archive | 2006
Patrick Mailliet; Luc Bertin; Didier Benard; Chantal Carrez; Francois Vallee; Eric Bacque
Archive | 2010
Luc Bertin; Jean-Christophe Carry; Patrick Mailliet; Hervé Minoux; Fabienne Pilorge; Jean-Marie Ruxer
Archive | 2006
Patrick Mailliet; Luc Bertin; Thierry Guyon; Fabienne Thompson; Jean-Marie Ruxer; Fabienne Pilorge; Didier Benard; Hervé Minoux; Chantal Carrez; Hélène Goulaouic
Archive | 2008
Luc Bertin; Chantal Carrez; Fabienne Thompson; Patrick Mailliet; Jean-Marie Ruxer
Archive | 2009
Jean Marie Ruxer; Patrick Mailliet; Jean Christophe Carry; Luc Bertin; Hervé Minoux