The discovery of colchicine-SAHA hybrids as a new class of antitumor agents |
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| Authors: | Xuan Zhang Jie Zhang Linjiang Tong Yu Luo Mingbo Su Yi Zang Jia Li Wei Lu Yi Chen |
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| 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;2. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, Shanghai 201203, PR China |
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| 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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| Keywords: | Colchicine SAHA HDAC Tubulin Hybrid |
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