Anti-tumor activity evaluation of novel tubulin and HDAC dual-targeting inhibitors.

Affiliation

Department of Medicinal Chemistry, School of Pharmacy, Qingdao University, Qingdao, Shandong, China. Electronic address: [Email]

Abstract

Histone deacetylases (HDACs) have proven to be promising targets for the development of anti-cancer drugs. In this study, we reported a series of novel chalcone based tubulin and HDAC dual-targeting inhibitors. Three compounds inhibited the activities of HDAC and tubulin polymerization simultaneously and displayed anti-proliferative activities toward eleven human tumor cell lines. Compound 8a remarkably induced growth inhibition, apoptosis and G2/M phase arrest of A549 tumor cells. Finally, the inhibitory activities of 8a against HDAC6 and tubulin were rationalized by molecular docking studies.

Keywords

Antitumor,Chalcone,Dual-targeting,Histone deacetylase,Inhibitor,Tubulin polymerization,

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