Michael Schnekenburger, Eric Goffin, Jin-Young Lee, Jun Young Jang, Aloran Mazumder, Seungwon Ji, Bernard Rogister, Nafila Bouider, Florence Lefranc, Walter Miklos, Véronique Mathieu, Pascal de Tullio, Kyu-Won Kim, Mario Dicato, Walter Berger, Byung Woo Han, Robert Kiss, Bernard Pirotte, Marc Diederich
A new series of N-aryl-N'-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)ureas bearing an alkoxycarbonylamino group at the 6-position were synthesized and examined as putative anticancer agents targeting sirtuins in glioma cells. On the basis of computational docking combined to in vitro sirtuin 1/2 inhibition assays, we selected compound 18 [R/S-N-3-cyanophenyl-N'-(6-tert-butoxycarbonylamino-3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-yl)urea] which displays a potent antiproliferative activity on various glioma cell types, assessed by quantitative videomicroscopy, eventually triggering senescence...
June 8, 2017: Journal of Medicinal Chemistry