title: Design, synthesis and evaluation of new 6-substituted-5-benzyloxy-4-oxo-4H-pyran-2-carboxamides as potential Src inhibitors.
abstract: Src family kinases (SFKs) are nonreceptor tyrosine kinases that are reported to be critical for cancer progression. Inhibiting the catalytic activity of these proteins has become one of the major therapeutic concepts in contemporary drug discovery. We report here the design and the synthesis of novel 6-substituted-5-benzyloxy-4-oxo-4H-pyran-2-carboxamides as potential inhibitors of Src kinase. The synthesis of these derivatives and the preliminary results of biological activity will be discussed.
authors.affiliation: Departement de Pharmacochimie, Faculté de Pharmacie, Université de Nantes, Nantes Atlantique Universites, Nantes, France. julien.farard@etu.univ-nantes.fr
authors.forename: Julien
authors.initials: J
authors.lastname: Farard
authors.forename: Gaëtan
authors.initials: G
authors.lastname: Lanceart
authors.forename: Cedric
authors.initials: C
authors.lastname: Logé
authors.forename: Marie-Reneé
authors.initials: MR
authors.lastname: Nourrisson
authors.forename: Francisco
authors.initials: F
authors.lastname: Cruzalegui
authors.forename: Bruno
authors.initials: B
authors.lastname: Pfeiffer
authors.forename: Muriel
authors.initials: M
authors.lastname: Duflos
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D020134:Catalytic Domain; D055808:Drug Discovery; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D019061:src-Family Kinases