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吡唑并喹啉酮类GSK-3抑制剂的合成及其细胞毒活性

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毗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。31p mol/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。
Syntheses and Cytotoxic Activities of Pyrazolo-Quinolinones GSK-3 Inhibitors
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 syntheses 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.

Pyrazolo-quinolinonesThree-component reactionGSK-3 inhibitorCytotoxic activityMolecular docking

黄正晓、张春菲、张春花、高慧、毛泽伟

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云南中医药大学中药学院 昆明 650500

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

国家自然科学基金项目云南省科学技术厅-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

82360842202101AZ070001-055202101AZ070001-043

2024

化学通报(印刷版)
中国科学院化学研究所 中国化学会

化学通报(印刷版)

CSTPCD北大核心
影响因子：0.547
ISSN：0441-3776
年,卷(期)：2024.87(10)