新型羽扇豆醇-3-脲/硫脲衍生物的设计、合成和抗肿瘤活性评估

IF 0.9 4区化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Russian Journal of General Chemistry Pub Date : 2024-11-19 DOI:10.1134/S1070363224100207

T. C. Xu, R. Luo, Z. X. Chen, J. Song, H. X. Cui, X. Hong, Y. L. Han, M. Bu, M. Wang

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引用次数: 0

摘要

研究人员设计、合成了一系列新型羽扇豆醇-3-脲/硫脲衍生物，并评估了它们对人肺癌 A549、人肝癌 HepG2 和人乳腺癌 MCF-7 细胞系的体外抗癌活性。所有化合物的抗肿瘤活性均高于母本露勃醇。其中，lup-20(29)-en-3β-yl-哌嗪羧酸-（2,4-氟苯基）脲对 A549 细胞株的抗肿瘤活性最强，IC50 为 3.22 μM，是羽扇豆醇的 10 倍。因此，lup-20(29)-en-3β-yl-哌嗪甲酸（2,4-氟苯基）脲可作为一种新的先导化合物，用于开发更强的抗肿瘤药物。

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Design, Synthesis, and Antitumor Activity Evaluation of Novel Lupeol-3-urea/thiourea Derivatives

A series of novel lupeol-3-urea/thiourea derivatives were designed, synthesized and evaluated for their in vitro anticancer activity against human lung cancer A549, human hepatocellular carcinoma HepG2 and human breast cancer MCF-7 cell lines. The antitumor activities of all compounds were higher than that of parent Lupeol. Among them, lup-20(29)-en-3β-yl-piperazinecarboxylate-(2,4-fluorophenyl)urea showed the strongest antitumor activity against A549 cell lines, with an IC₅₀ of 3.22 μM, which is tenfold than that of Lupeol. Therefore, lup-20(29)-en-3β-yl-piperazinecarboxylate-(2,4-fluorophenyl)urea can be used as a new lead compound for the development of more potent antitumor drugs.

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来源期刊

Russian Journal of General Chemistry 化学-化学综合

CiteScore

1.40

自引率

22.20%

发文量

252

审稿时长

2-4 weeks

期刊介绍： Russian Journal of General Chemistry is a journal that covers many problems that are of general interest to the whole community of chemists. The journal is the successor to Russia’s first chemical journal, Zhurnal Russkogo Khimicheskogo Obshchestva (Journal of the Russian Chemical Society ) founded in 1869 to cover all aspects of chemistry. Now the journal is focused on the interdisciplinary areas of chemistry (organometallics, organometalloids, organoinorganic complexes, mechanochemistry, nanochemistry, etc.), new achievements and long-term results in the field. The journal publishes reviews, current scientific papers, letters to the editor, and discussion papers.