| 新型1,3-二取代酞嗪酮类衍生物的合成及抗肿瘤活性研究 |
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| 引用本文： | 张路野,张洋,包崇男,杨鹏,李二冬,孟娅琪,崔飞,周蕊,黄诗雨,郑甲信,单丽红,刘宏民,张秋荣.新型1,3-二取代酞嗪酮类衍生物的合成及抗肿瘤活性研究[J].有机化学,2020(3):794-800. |
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| 作者姓名： | 张路野 张洋 包崇男 杨鹏 李二冬 孟娅琪 崔飞 周蕊 黄诗雨 郑甲信 单丽红 刘宏民 张秋荣 |
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| 作者单位： | 郑州大学药学院;新药创制与药物安全性评价河南省协同创新中心;省部共建食管癌防治国家重点实验室;教育部药物制备关键技术重点实验室 |
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| 基金项目： | 国家自然科学基金(No.81430085);河南省自然科学基金(No.182300410321);省部共建食管癌防治国家重点实验室开放基金(No.K2020000X)资助项目. |
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| 摘 要： | 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6.01μmol/L,为抗肿瘤药物的研究提供了思路.
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| 关 键 词： | 酞嗪 衍生物 合成 抗增殖活性 |
Synthesis and Antitumor Activity of Novel 1,3-Disubstituted Pyridazinone Derivatives |
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| Zhang Luye,Zhang Yang,Bao Chongnan,Yang Peng,Li Erdong,Meng Yaqi,Cui Fei,Zhou Rui,Huang Shiyu,Zheng Jiaxin,Shan Lihong,Liu Hongmin,Zhang Qiurong.Synthesis and Antitumor Activity of Novel 1,3-Disubstituted Pyridazinone Derivatives[J].Chinese Journal of Organic Chemistry,2020(3):794-800. |
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| Authors: | Zhang Luye Zhang Yang Bao Chongnan Yang Peng Li Erdong Meng Yaqi Cui Fei Zhou Rui Huang Shiyu Zheng Jiaxin Shan Lihong Liu Hongmin Zhang Qiurong |
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| Institution: | (School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001;Collaborative Innovation Center of New Drug Research and Safety Evaluation,Zhengzhou 450001;State Key Laboratorv of Esophageal Cancer Prevention&Treatment,Zhengzhou University Zhengzhou 450052;Key Laboratory of Advanced Drug Preparation Technologies,Ministry of Education of China,Zhengzhou 450001) |
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| Abstract: | 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)-7V-(2-fluorophenyl)acetamide(5g)exhibited better antiproliferative activities with IC50 value of 6.01μmol/L.In a nutshell,this work provided clues to discover antitumor agent based on the quinazoline scaffold. |
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| Keywords: | pyridazinederiv ative synthesis antiproliferative activity |
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