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Design, synthesis, and cytotoxic activities of novel hybrids of parthenolide and thiazolidinedione via click chemistry.
Journal of Asian Natural Products Research ( IF 1.7 ) Pub Date : 2019-04-23 , DOI: 10.1080/10286020.2019.1597055
Jie Qiu 1, 2, 3 , Chun-Mao Yuan 1, 2, 3 , Min Wen 1, 3 , Ya-Nan Li 1, 2, 3 , Juan Chen 1, 2, 3 , Jun-You Jian 1, 2, 3 , Lie-Jun Huang 1, 2, 3 , Wei Gu 1, 2, 3 , Yan-Mei Li 1, 2, 3 , Xiao-Jiang Hao 1, 2, 3, 4
Affiliation  

A series of novel parthenolide-thiazolidinedione hybrids have been synthesized via a click chemistry-mediated coupling between parthenolide and thiazolidinedione, and evaluated for their cytotoxic activities. The results indicated that all the hybrids showed moderate cytotoxic effects on human cancer cell lines, including human erythroleukemia cell line (HEL), prostate (PC3), and breast (MDA-MB-231) by MTT assay. In particular, compound VI-6 exhibited the best cytotoxic activities against the MDA-MB-231 cells with IC50 value of 2.07 µM, which was about eight times more active than that of the original compound (PTL). These interesting results might be used to develop novel lead scaffolds for potential anticancer agents.

中文翻译:

通过点击化学方法,设计了新的白菊内酯和噻唑烷二酮杂化物,并对其进行了细胞毒性研究。

已经通过点击化学介导的帕特诺尔内酯和噻唑烷二酮之间的偶联合成了一系列新颖的帕特诺尔内酯-噻唑烷二酮杂合物,并对其细胞毒性进行了评估。结果表明,通过MTT分析,所有杂种均对人癌细胞系包括人红白血病细胞系(HEL),前列腺(PC3)和乳腺(MDA-MB-231)表现出中等的细胞毒性作用。特别是,化合物VI-6对MDA-MB-231细胞表现出最佳的细胞毒活性,IC50值为2.07 µM,是原始化合物(PTL)活性的约八倍。这些有趣的结果可用于开发潜在的抗癌药物的新型铅支架。
更新日期:2020-04-20
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