摘要/Abstract

为了寻找高效低毒的抗肿瘤药物，设计并合成新型的1，3位取代酞嗪酮类化合物.采用噻唑蓝（MTT）法对目标化合物在MCF-7（人乳腺癌细胞）、PC-3（人前列腺癌细胞）、SW-620（人结肠癌细胞）和HGC-27（人胃癌细胞）四种人类癌细胞的抗增殖活性进行评价.结果显示大部分化合物具有较好的抗增殖活性.其中，2-（4-（4-溴苯基）-1-氧代酞嗪-2（1H）-基）-N-（2-氟苯基）乙酰胺（5g）对MCF-7细胞的抗增殖活性较好，IC₅₀值为6.01 μmol/L，为抗肿瘤药物的研究提供了思路.
关键词: 酞嗪, 衍生物, 合成, 抗增殖活性
In order to find more efficient and low toxicity antitumor drugs, a series of novel 1,3-disubstituted pyridazinone derivatives were synthesized and evaluated for their antiproliferative activities against four human cancer cell lines (MCF-7, PC-3, SW-620 and HGC-27) in vitro. The results showed that most compounds had good antiproliferative activities, especially 2-(4-(4-bromophenyl)-1-oxo-tolylazine-2(1H)-yl)-N-(2-fluorophenyl)acetamide (5g) exhibited better antiproliferative activities with IC₅₀ value of 6.01 μmol/L. In a nutshell, this work provided clues to discover antitumor agent based on the quinazoline scaffold.
Key words: pyridazinederiv, ative, synthesis, antiproliferative activity


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