2. Academic Validation
  3. Novel N-phenyl dichloroacetamide derivatives as anticancer reagents: design, synthesis and biological evaluation

Novel N-phenyl dichloroacetamide derivatives as anticancer reagents: design, synthesis and biological evaluation

  • Eur J Med Chem. 2010 Sep;45(9):4300-6. doi: 10.1016/j.ejmech.2010.06.032.
Yongchong Yang 1,  Peihua Shang,  Changmei Cheng,  Dongchun Wang,  Ping Yang,  Feng Zhang,  Tianwen Li,  Aijun Lu,  Yufen Zhao
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: 20663593 DOI: 10.1016/j.ejmech.2010.06.032
Abstract

A current study shows that sodium dichloroacetate (DCA) can induce Cancer cell Apoptosis and inhibit tumor growth, but its cytotoxic activity is low (IC(50) > 1000 microM for A549). In this paper, a variety of DCA derivatives were synthesized, and their cytotoxic activities were evaluated. The result showed that the N-phenyl-2,2-dichloroacetamide analogues had satisfactory potencies. Among them, N-(3-iodophenyl)-2,2-dichloroacetamide (3e), an optimized lead compound, has an IC(50) against A549 as low as 4.76 microM. Furthermore, it can induce Cancer cell Apoptosis and has a low toxicity in mice (LD(50) = 1117 mg/kg).

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