Design, synthesis and evaluation of new 6-substituted-5-benzyloxy-4-oxo-4H-pyran-2-carboxamides as potential Src inhibitors.
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.
Farard
Julien
J
Departement de Pharmacochimie, Faculté de Pharmacie, Université de Nantes, Nantes Atlantique Universites, Nantes, France. julien.farard@etu.univ-nantes.fr
Lanceart
Gaëtan
G
Logé
Cedric
C
Nourrisson
Marie-Reneé
MR
Cruzalegui
Francisco
F
Pfeiffer
Bruno
B
Duflos
Muriel
M
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*
D000577:Amides; D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D019061:src-Family Kinases