Imidazopyridine-fused [1,3]-diazepinones: Synthesis and antiproliferative activity. - Archive ouverte HAL
Article Dans Une Revue European Journal of Medicinal Chemistry Année : 2014

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

Résumé

: 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
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Dates et versions

hal-00952223 , version 1 (26-02-2014)

Identifiants

Citer

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⟩
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