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目的设计合成一系列46,-双苯基-2-氨基-3-氰基吡啶类化合物,并对其体外抗肿瘤活性进行初步评价。方法以取代苯甲醛、取代苯乙酮、丙二腈和醋酸铵为原料,经一步反应制得目标化合物。采用MTT法,以MX-58151为阳性对照药,以A549、HT-29和SMMC-7721为测试细胞株对目标化合物进行体外抗肿瘤活性评价。结果与结论合成了13个未见报道的46,-双苯基-2-氨基-3-氰基吡啶类化合物,其结构经1H-NMR、MS和IR谱确证。体外活性测试结果显示,多数化合物能够在较低的浓度下抑制肿瘤细胞增殖。其中,2-氨基-6-(4-氟苯基)-4-(23,,4-三甲氧基苯基)-3-氰基吡啶具有显著的抗肿瘤细胞增殖活性I,C50值达纳摩尔级水平,明显优于阳性对照药MX-58151。
OBJECTIVE To design and synthesize a series of 46, - bis-phenyl-2-amino-3-cyanopyridines and to evaluate their anti-tumor activity in vitro. Methods The target compounds were prepared by one step reaction using substituted benzaldehyde, substituted acetophenone, malononitrile and ammonium acetate as raw materials. MTT assay was used to evaluate the antitumor activity of the target compounds in vitro using MX-58151 as a positive control drug and A549, HT-29 and SMMC-7721 as test cell lines. RESULTS AND CONCLUSION Thirteen new reported 46-bis-phenyl-2-amino-3-cyanopyridines were synthesized and their structures were confirmed by 1H-NMR, MS and IR spectra. In vitro activity test results show that most compounds can inhibit tumor cell proliferation at lower concentrations. Among them, 2-amino-6- (4-fluorophenyl) -4- (23,4-trimethoxyphenyl) -3-cyanopyridine has significant anti-tumor cell proliferation activity Moore’s level, significantly better than the positive control drug MX-58151.