Gallud Audrey, Vaillant Ophélie, Maillard Ludovic T, Arama Dominique P, Dubois Joëlle, Maynadier Marie, Lisowski Vincent, Garcia Marcel, Martinez Jean, Masurier Nicolas
Institut des Biomolécules Max Mousseron, UMR 5247, CNRS, Universités Montpellier I et II, UFR des Sciences Pharmaceutiques et Biologiques, 15 Avenue Charles Flahault, 34093 Montpellier Cedex 5, France.
Institut de Chimie des Substances Naturelles, UPR 2301 CNRS, Centre de Recherche de Gif, Avenue de la Terrasse, F-91198 Gif-sur-Yvette Cedex, France.
Eur J Med Chem. 2014 Mar 21;75:382-90. doi: 10.1016/j.ejmech.2014.01.044. Epub 2014 Jan 30.
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.
合成了一系列15种吡啶并咪唑并-1,3-二氮杂卓-5-酮和吡啶并-1,3-二氮杂卓-2,5-二酮，并评估了它们的抗癌活性。在一组细胞系上测试的化合物中，化合物6a对21种细胞系表现出最佳的生长抑制活性，对MDA-MB-435黑色素瘤细胞具有细胞毒性作用。该化合物导致细胞形态发生深刻变化，并且被发现是肝细胞祖激酶样激酶（HGK）的抑制剂，已知该激酶与各种肿瘤细胞的迁移、粘附和侵袭有关。
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