Synthesis and Antitumor Activity of Erlotinib Derivatives Linked With 1,2,3-Triazole

文献类型： 外文期刊

第一作者： Deng, Peng

作者： Deng, Peng;Peng, Lizeng;Mao, Longfei;Sun, Ge;Yao, Kaitai;Zhao, Jie;Yuan, Miaomiao

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关键词： EGFR; erlotinib; 1; 2; 3-triazole; HeLa; antitumor activity

期刊名称：FRONTIERS IN PHARMACOLOGY （ 影响因子：5.811； 五年影响因子：6.006 ）

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年卷期： 2022 年 12 卷

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收录情况： SCI

摘要： Cervical cancer is one of the most important cause of cancer-related death and presents a major public health problem in many countries. To search for more novel antitumor agents against cervical cancer, 14 erlotinib-linked 1,2,3-triazole compounds were designed, synthesized, and evaluated for their anti-tumor activity. The compounds were confirmed by H-1 NMR, C-13 NMR, and high-resolution mass spectra (HR MS). Antitumor activity assay results indicated that six of those compounds have remarkable inhibitory activity against human cervical cancer HeLa cells in vitro, among which compound 4m was the most potent with IC50 of 3.79 mu M, and compounds 4k, 4i, 4l, 4d, and 4n also demonstrated remarkable antitumor activity with IC50 of 3.79, 4.16, 4.36, 7.02, and 8.21 mu M. We found three of the most potent compounds 4d, 4k, and 4l induced potent apoptosis and cell cycle arrest in HeLa cells, and compounds 4d and 4l significantly restrained the cell colony formation and showed moderate epidermal growth factor receptor (EGFR) inhibitory activity with IC50 of 13.01 and 1.76 mu M. Therefore, these experiments indicate that these erlotinib-linked 1,2,3-triazole compounds are potential to act as effective anticancer agents against cervical cancer.

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