Design,synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents |
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| Authors: | Tianwen Li Yongchong Yang Changmei Cheng Amit K Tiwari Kamlesh Sodani Yufen Zhao Ioana Abraham Zhe-Sheng Chen |
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| Institution: | 1. Key laboratory of Bioorganic Phosphorus and Chemical Biology, The Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, PR China;2. Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John’s University, Queen, NY 11439, USA |
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| Abstract: | Our earlier research has shown that N-phenyl-2,2-dichloroacetamide analogues had much higher anti-cancer activity than the lead compound sodium dichloroacetate (DCA). In this current study, a variety of N-arylphenyl-2,2-dichloroacetamide analogues were synthesized via Suzuki coupling reaction and their anti-cancer activity was evaluated. The results showed that N-terphenyl-2,2-dichloroacetamide analogues had satisfactory anti-cancer activity. Among them, N-(3,5-bis(benzod]1,3]dioxol-5-yl)phenyl)-2,2-dichloroacetamide (6 k) had an IC50 of 2.40 μM against KB-3-1 cells, 1.04 μM against H460 cells and 1.73 μM against A549 cells. |
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