Synthesis of selenophene-based chalcone analogs and assessment of their biological activity as anticancer agents

被引:3
|
作者
Chen, Ya-Chen [1 ]
Li, Cai-Wei [2 ]
Chen, Jih-Jung [3 ,4 ]
Shih, Tzenge-Lien [1 ]
机构
[1] Tamkang Univ, Dept Chem, New Taipei 251301, Taiwan
[2] Natl Yang Ming Chiao Tung Univ, Inst Tradit Med, Taipei, Taiwan
[3] Natl Yang Ming Chiao Tung Univ, Coll Pharmaceut Sci, Dept Pharm, Taipei 112304, Taiwan
[4] China Med Univ Hosp, China Med Univ, Dept Med Res, Taichung, Taiwan
关键词
anticancer; chalcone; human colorectal adenocarcinoma cell; selenophene; GLUTATHIONE-PEROXIDASE; ANTIOXIDANT ACTIVITY; SELENIUM; EBSELEN; ORGANOSELENIUM; DISEASE; DEFICIENCY; PREVENTION; MECHANISM; COMPOUND;
D O I
10.1002/ardp.202200486
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Selenium is an essential micronutrient that is beneficial to human health. Selenium-containing drugs have been developed as antioxidants, anti-inflammatory, and anticancer agents. However, the synthesis of selenium-containing chalcones has not been fully explored. Therefore, we report the synthesis of novel selenophene-based chalcone analogs and reveal their biological activities as anticancer agents. Among the seven synthesized molecules, compounds 6, 8, and 10 exhibited anticancer activity with IC50 values of 19.98 +/- 3.38, 38.23 +/- 3.30, and 46.95 +/- 5.68 mu M, respectively, against human colorectal adenocarcinoma (HT-29) cells. Clonogenic assays and Western blot analysis tests further confirmed that compound 6 effectively induced apoptosis in HT-29 cells through mitochondrial- and caspase-3-dependent pathways.
引用
收藏
页数:8
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