2. Academic Validation
  3. The discovery of colchicine-SAHA hybrids as a new class of antitumor agents

The discovery of colchicine-SAHA hybrids as a new class of antitumor agents

  • Bioorg Med Chem. 2013 Jun 1;21(11):3240-4. doi: 10.1016/j.bmc.2013.03.049.
Xuan Zhang 1,  Jie Zhang,  Linjiang Tong,  Yu Luo,  Mingbo Su,  Yi Zang,  Jia Li,  Wei Lu,  Yi Chen
Affiliations

Affiliation

  • 1 Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.
PMID: 23602523 DOI: 10.1016/j.bmc.2013.03.049
Abstract

A novel class of colchicine-SAHA hybrids were designed and synthesised based on the synergistic antitumor effect of tubulin inhibitors and histone deacetylases (HDAC) inhibitors. To the best of our knowledge, this is the first design of molecules that are dual inhibitors of tubulin and HDAC. Biological evaluations of these compounds included the inhibitory activity of HDAC, in vitro cell cycle analysis in BEL-7402 cells as well as cytotoxicity in five Cancer cell lines.

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