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根据拼药原理,将氮芥类抗肿瘤药物的药效基团N,N-二(2-氯乙基)氨基拼接到查尔酮结构中,合成出了一系列新型含氮芥基的查尔酮衍生物3a～3r,并用1H NMR,IR,HRMS-ESI及X射线对其结构进行了确证.采用MTT法对所合成的化合物进行了体外抗肿瘤活性测试,结果表明部分化合物对所选肿瘤细胞的增殖有较强的抑制作用,其中,化合物3j和3l对K562的IC50值分别为20.01和18.6μmol/L;对HepG2的IC50值分别为43.46和21.39μmol/L.实验培养并得到了目标产物3e和3l的晶体结构,X射线分析表明化合物3e和3l都属三斜晶系,P-1空间群.
According to the spelling principle, the pharmacophore group N, N-bis (2-chloroethyl) amino group of the nitrogen mustard anticancer drug is spliced into the chalcone structure to synthesize a series of new nitrogen-containing mustard And their structures were confirmed by 1H NMR, IR, HRMS-ESI and X-ray.The in vitro antitumor activity of the synthesized compounds was tested by MTT method and the results showed that some of the compounds were selected for the selected The IC50 values of compound 3j and 3l to K562 were 20.01 and 18.6μmol / L, respectively, and the IC50 values of HepG2 were 43.46 and 21.39μmol / L respectively.Experimental culture and obtained The crystal structure of the target products 3e and 3l, X-ray analysis showed that compounds 3e and 3l belong to the triclinic, P-1 space group.