摘要/Abstract

为了寻求高效的新型抗肿瘤药物，设计并合成了一系列新型2-甲硫基-4-苯胺喹唑啉衍生物，对这些化合物在人类四种癌细胞MGC-803（人胃癌细胞）、PC-3（人前列腺癌细胞）、HGC-27（人胃癌细胞）和A549（人非小细胞肺癌细胞）进行抗肿瘤活性评价.结果显示部分化合物具有较好的抗肿瘤活性，其中N-（4-氟苯基）-2-（甲硫基）喹唑啉-4-胺（9c）和N-（4-甲基苯基）-2-（甲硫基）喹唑啉-4-胺（9m）显示出较高的抗肿瘤活性，IC₅₀值分别为0.18和0.68 μmol·L^-1.
关键词: 喹唑啉衍生物, 合成, 抗肿瘤活性, 评价
In order to find the efficient and novel antitumor drugs, a series of 2-methylthio-4-arylamine quinazoline derivatives were designed and synthesized. The target compounds were evaluated for antitumor activity in vitro on four human cancer cell lines initially including MGC-803, PC-3, HGC-27 and A549. The results showed that some compounds had good antitumor activities, especially N-(4-fluorophenyl)-2-(methylthio) quinazolin-4-amine (9c) and 2-(methylthio)-N-(p-tolyl)-quina-zolin-4-amine (9m), with IC₅₀ values of 0.18 and 0.68 μmol·L^-1, respectively.
Key words: quinazoline derivatives, synthesis, antitumor activity, evaluation


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