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1,3,5-Triazine inhibitors of histone deacetylases: synthesis and biological activity

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Abstract

A series of 1,3,5-triazine-based hydroximic acids 6a6i were designed and synthesized, and they were found to be potent inhibitors of human histone deacetylases. These compounds were evaluated for their antiproliferative activity by MTT assay, and most of them exhibited significant antiproliferative effect on HCT-116, MCF-7, and HeLa cancer cell lines. DNA flow cytometric analysis revealed that compound 6i induced apoptosis and cell cycle arrest at G2/M phase in HCT-116 cells.

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Acknowledgments

These studies in the laboratories were supported by the natural science foundation of Jiangsu Province (BK2011390), Priority Academic Program Development of Jiangsu Higher Education Instititutions (PAPD).

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Correspondence to Yu Zhao.

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Zhao, X., Tan, Q., Zhang, Z. et al. 1,3,5-Triazine inhibitors of histone deacetylases: synthesis and biological activity. Med Chem Res 23, 5188–5196 (2014). https://doi.org/10.1007/s00044-014-1084-z

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  • DOI: https://doi.org/10.1007/s00044-014-1084-z

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