Imidazopyridine-fused [1,3]-diazepinones: Synthesis and antiproliferative activity.

Audrey Gallud (1) , Ophélie Vaillant (1) , Ludovic T Maillard (1) , Dominique P Arama (1) , Joëlle Dubois (2) , Marie Maynadier (1) , Vincent Lisowski (1) , Marcel Garcia (1) , Jean Martinez (1) , Nicolas Masurier (1)

1 IBMM - Institut des Biomolécules Max Mousseron [Pôle Chimie Balard]
2 ICSN - Institut de Chimie des Substances Naturelles

: A series of 15 pyrido-imidazo-1,3-diazepin-5-ones and pyrido-1,3-diazepine-2,5-diones were synthesized and their anticancer activities were evaluated. Among tested compounds on a cell lines panel, compound 6a presents the best growth inhibition activity on 21 cell lines with a cytotoxic effect on MDA-MB-435 melanoma cells. This compound led to deep cell morphological changes and revealed to be an inhibitor of the Hepatocyte progenitor kinase-like kinase (HGK), which is known to be implicated in the migration, adhesion and invasion of various tumor cells.

Domaines: Chimie organique

Audrey Gallud, Ophélie Vaillant, Ludovic T Maillard, Dominique P Arama, Joëlle Dubois, et al.. Imidazopyridine-fused [1,3]-diazepinones: Synthesis and antiproliferative activity.. European Journal of Medicinal Chemistry, 2014, 75C, pp.382-390. ⟨10.1016/j.ejmech.2014.01.044⟩. ⟨hal-00952223⟩