- 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.
European journal of medicinal chemistry (2010-07-29)
Yongchong Yang, Peihua Shang, Changmei Cheng, Dongchun Wang, Ping Yang, Feng Zhang, Tianwen Li, Aijun Lu, Yufen Zhao
PMID20663593
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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