摘要/Abstract

为了寻找高效的新型抗肿瘤药物，设计并合成了一系列新型腙基取代的2，4，6-取代嘧啶衍生物，并对目标化合物在MCF-7（人乳腺癌细胞），MGC-803（人胃癌细胞系），PC-3（人前列腺癌细胞），Hela（人宫颈癌细胞）和A549（人肺癌细胞）进行抗肿瘤活性评价.结果显示部分化合物对PC-3表现出中度至强效的抗肿瘤活性.其中2-（丙-2-炔-1-基硫基）-4-（2-（吡啶-2-基亚甲基）-肼基）-6-（三氟甲基）嘧啶（12l）对PC-3具有较强的抗增殖活性，IC₅₀为1.37 μmol·L^-1，抗肿瘤活性明显优于阳性对照药5-氟尿嘧啶，为抗肿瘤药物的研究提供了新的思路.
关键词: 腙, 嘧啶衍生物, 合成, 抗肿瘤活性
In order to find more effective antitumor drugs, a series of novel hydrazone-substituted pyrimidine derivatives were designed, synthesized and evaluated for their antitumor activity against five different human cancer cell lines including MCF-7 (human breast cancer cell), MGC-803 (human gastric cancer cell), PC-3 (human prostate cancer cell), Hela (human cervical cancer cell) and A549 (human lung cancer cell) using methyl thiazolyl tetrazolium (MTT) assay. Most of the target compounds showed moderate to potent antitumor activity against five selected cancer cell lines. Among them, 2-(prop-2-yn-1-ylthio)-4-(2-(pyridin-2-ylmethylene)-hydrazinyl)-6-(trifluoromethyl)pyrimidine (12l) displayed the most potent anti-proliferative activity against PC-3 cell line (IC₅₀=1.37 μmol·L^-1), which was significantly better than the positive control drug 5-fluorouracil. This work provided clues to discover new antitumor agents.
Key words: hydrazone, pyrimidine derivatives, synthesis, antitumor activity


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