17090-46-9Relevant academic research and scientific papers
Novel N-phenyl dichloroacetamide derivatives as anticancer reagents: Design, synthesis and biological evaluation
Yang, Yongchong,Shang, Peihua,Cheng, Changmei,Wang, Dongchun,Yang, Ping,Zhang, Feng,Li, Tianwen,Lu, Aijun,Zhao, Yufen
experimental part, p. 4300 - 4306 (2010/10/02)
A current study shows that sodium dichloroacetate (DCA) can induce cancer cell apoptosis and inhibit tumor growth, but its cytotoxic activity is low (IC50 > 1000 μM 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 IC50 against A549 as low as 4.76 μM. Furthermore, it can induce cancer cell apoptosis and has a low toxicity in mice (LD50 = 1117 mg/kg). N-phenyl-2,2-dichloroacetamide analogues has higher cytotoxic activity and N-(3-iodophenyl)-2,2-dichloroacetamide (3e) is an optimized lead compound.
