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Development of Novel Thiazolopyrimidines as CDC25B Phosphatase Inhibitors |
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| Authors: | Stéphanie Kolb Odile Mondésert Mary‐Lorène Goddard Dr. Denis Jullien Dr. Bruno O. Villoutreix Dr. Bernard Ducommun Prof. Christiane Garbay Prof. Emmanuelle Braud Dr. |
| Affiliation: | 1. Université Paris Descartes, UFR Biomédicale, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, 45 Rue des Saints Pères, 75270 Paris Cedex 06 (France), Fax: (+33)?142‐864‐082;2. INSERM U648, 45 Rue des Saints Pères, 75270 Paris Cedex 06 (France);3. Université de Toulouse, LBCMCP, 118 Route de Narbonne, 31062 Toulouse (France);4. CNRS, LBCMCP – UMR5088, 31062 Toulouse (France);5. INSERM U973, Université Paris Diderot Lamarck, 75013 Paris (France);6. CHU Purpan, TSA 40031, 31059 Toulouse (France) |
| Abstract: | CDC25 inhibition by thiazolopyrimidines : CDC25 is an attractive target for cancer therapy, as it is overexpressed in numerous cancers and is often associated with tumor aggressiveness and poor prognosis. Based on an in silico/in vitro screen, we developed a series of thiazolopyrimidines to further improve inhibitory activity and cytotoxic properties.  |
| Keywords: | cancer CDC25 phosphatase cell cycle structure– activity relationships thiazolopyrimidines |