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

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

  • Bioorg Med Chem Lett. 2019 Sep 15;29(18):2638-2645. doi: 10.1016/j.bmcl.2019.07.045.
Baolei Wang 1,  Xuehong Chen 2,  Jianjun Gao 3,  Li Su 1,  Li Zhang 1,  Hongwei Xu 2,  Yepeng Luan 4
Affiliations

Affiliations

  • 1 Department of Medicinal Chemistry, School of Pharmacy, Qingdao University, Qingdao, Shandong, China.
  • 2 Department of Pharmacology, College of Basic Medicine, Qingdao University, Qingdao, Shandong, China.
  • 3 Department of Pharmacology, School of Pharmacy, Qingdao University, Qingdao, Shandong, China.
  • 4 Department of Medicinal Chemistry, School of Pharmacy, Qingdao University, Qingdao, Shandong, China. Electronic address: luanqdu@sina.com.
PMID: 31400938 DOI: 10.1016/j.bmcl.2019.07.045
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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