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目的设计并合成2-取代-4-氨基噻吩并[3,2-d]嘧啶类化合物,评价其体外抗增殖活性。方法以3-氨基-2-噻吩甲酸甲酯为起始原料,经6步反应合成目标化合物;以CP-31398为阳性对照药,采用MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide]法测定了目标化合物对肿瘤细胞株H-460和HT-29的抗增殖活性。结果与结论合成16个未见文献报道的化合物,其结构经1H-NMR、MS确证;5个化合物显示较好的抗增殖活性,其中,化合物8n活性突出,为CP-31398的4-5倍。
Objective To design and synthesize 2-substituted-4-aminothieno [3,2-d] pyrimidines and evaluate their in vitro antiproliferative activity. Methods The title compound was synthesized via 6 steps using methyl 3-amino-2-thiophenecarboxylate as starting material. CP-31398 was used as a positive control and MTT [3- (4,5-dimethylthiazol-2-yl) -2,5-diphenyltetrazolium bromide] method was used to determine the antiproliferative activity of the target compounds against tumor cell lines H-460 and HT-29. RESULTS AND CONCLUSION Sixteen compounds were synthesized and their structures were confirmed by 1H-NMR and MS. Five compounds showed good antiproliferative activity. Among them, the activity of 8n was prominent, which was 4-5 times that of CP-31398 .