2. Academic Validation
  3. Design, synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents

Design, synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents

  • Bioorg Med Chem Lett. 2012 Dec 1;22(23):7268-71. doi: 10.1016/j.bmcl.2012.07.057.
Tianwen Li 1,  Yongchong Yang,  Changmei Cheng,  Amit K Tiwari,  Kamlesh Sodani,  Yufen Zhao,  Ioana Abraham,  Zhe-Sheng Chen
Affiliations

Affiliation

  • 1 Key Laboratory of Bioorganic Phosphorus and Chemical Biology, The Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, PR China.
PMID: 23067553 DOI: 10.1016/j.bmcl.2012.07.057
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(benzo[d][1,3]dioxol-5-yl)phenyl)-2,2-dichloroacetamide (6 k) had an IC(50) 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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