多取代N-苯基-二氯乙酰胺类抗癌药物：设计、合成、生物活性评价(英文)

Multi-substituted N-phenyl-2,2-dichloroacetamide analogues as anti-cancer drugs:design,synthesis and biological evaluation

根据早期研究发现的单取代N-苯基-二氯乙酰胺类化合物比先导化合物二氯乙酸钠(DCA)具有更高抗癌活性的研究结果,本文合成了系列多取代N-苯基-二氯乙酰胺类化合物并对其进行生物活性评价,结果显示3,5-二取代-N-苯基-二氯乙酰胺类化合物表现出更高的活性,其中N-(3,5-二碘-苯基)-二氯乙酰胺抑制非小细胞肺癌细胞株(A549)的IC50为2.84μmol.L-1,且能够诱导癌细胞凋亡。

Our earlier research has shown that mono-substituted N-phenyl-2,2-dichloroacetamide exhibited much higher anti-cancer activity than the lead compound sodium dichloroacetate（DCA）.In this paper,a variety of multi-substituted N-phenyl-2,2-dichloroacetamides were synthesized and biologically evaluated.The results showed that 3,5-disubstituted N-phenyl-2,2-dichloroacetamide analogues had satisfactory potency.Among them,N-（3,5-diiodophenyl）-2,2-dichloroacetamide had an IC50 of 2.84 μmol·L-1 against non-small cell lung cancer cell line A549 and could induce cancer cell apoptosis.