黄正晓,张春菲,张春花,高慧,毛泽伟.化学通报,2024,87(10):11229-1233.
吡唑并喹啉酮类GSK-3抑制剂的合成及其细胞毒活性
Synthesis and cytotoxic activity of pyrazolo-quinolinones GSK-3 inhibitors
投稿时间:2024-05-27  修订日期:2024-07-24
DOI:
中文关键词:  吡唑并喹啉酮  三组分反应  GSK-3抑制剂  细胞毒活性  分子对接
英文关键词:Pyrazolo-quinolinones  three-component reaction  GSK-3 inhibitor  cytotoxic activity  molecular docking
基金项目:国家自然科学基金项目(82360842)和云南省科学技术厅-云南中医药大学应用基础研究联合专项项目(202101AZ070001-055,202101AZ070001-043)资助
作者单位E-mail
黄正晓 云南中医药大学中药学院 hzx2056900191@163.com 
张春菲 云南中医药大学中药学院  
张春花 云南中医药大学中药学院  
高慧 云南中医药大学中药学院  
毛泽伟* 云南中医药大学中药学院 maozw@ynucm.edu.cn 
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中文摘要:
      吡唑并喹啉酮是一类具有抗肿瘤、抗氧化等多种生物活性的新型化合物,具有很好的药用前景,然而目前对该类化合物的合成及生物活性报道较少。本论文采用三组分“一锅法”合成得到8个吡唑并喹啉酮衍生物(a-h),并对其体外细胞毒活性进行了初步评价。结果发现,化合物对肿瘤细胞株Hela、HCC1806和A549表现出较好的选择性抑制活性,特别是化合物h对A549的抑制作用最强(IC50=1.31 μmol/L)。分子对接结果显示,化合物h与靶点蛋白4PTC之间存在较强的结合作用,可作为潜在的糖原合成酶激酶-3(GSK-3)抑制剂进行深入研究。
英文摘要:
      Pyrazolo-quinolinones is a new class of compounds with anti-tumor, anti-oxidation and other biological activities, which has a good medicinal prospect. However, there are few reports on the synthesis and biological activities of these compounds. In this paper, eight Pyrazolo-quinolinones derivatives (a-h) have been prepared by a three-component "one-pot" reaction, and their cytotoxic activities were evaluated. The results showed that the compounds exhibited good selective cytotoxic activity against tumor cell lines (Hela, HCC1806 and A549), especially compound h showed the best inhibitory effect on A549 (IC50=1.31 μmol/L). In addition, the molecular docking study indicated that compound h had a strong interaction with the target protein 4PTC, which could be considered as potential glycogen synthase kinase-3 inhibitor for further study.
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