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

Abstract

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.

Keywords: Antitumor activity; Diazepinones; HGK inhibitors; Imidazo[1,2-a]pyridine; Polyfused heterocycles.