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目的合成N-(2,3-二甲基-2H-吲唑-6-基)-2-甲基嘧啶二胺衍生物,测试所合成化合物的体外抗肿瘤活性。方法在已上市的多靶点小分子抗肿瘤药pazopanib的构效关系基础上,采用基于片段的药物设计方法设计合成目标化合物;采用四氮唑盐(MTT)法测试所合成化合物的体外抗肿瘤活性。结果合成了14个N-(2,3-二甲基-2H-吲唑-6-基)-2-甲基嘧啶二胺衍生物,目标化合物的结构经1H-NMR、MS及元素分析确证。结论大多数合成的化合物表现出一定的抗肿瘤活性,其中化合物B1和B2的抗肿瘤活性优于阳性对照。
Aim To synthesize N- (2,3-dimethyl-2H-indazol-6-yl) -2-methylpyrimidinediamine derivatives and test the antitumor activity of the synthesized compounds in vitro. Methods Based on the structure-activity relationship of pazopanib, a multi-target small molecule antitumor drug on the market, the target compound was designed and synthesized by fragment-based drug design method. The antitumor activity of the synthesized compounds was tested by MTT assay active. Results Fourteen N- (2,3-dimethyl-2H-indazol-6-yl) -2-methylpyrimidinediamine derivatives were synthesized. The structures of the target compounds were confirmed by 1H-NMR, MS and elemental analysis . Conclusion Most of the synthesized compounds showed some anti-tumor activity, of which compounds B1 and B2 had better anti-tumor activity than the positive control.