Synthesis and in vitro antitumor activity of (1E, 4E)-1-aryl-5-(2-(( quinazolin-4-yl) oxy) phenyl)-1,4-pentadien-3-one derivatives
文献类型： 外文期刊
作者： Luo, Hui 1 ; Yang, Shengjie 2 ; Hong, Da 2 ; Xue, Wei 3 ; Xie, Pu 1 ;
作者机构： 1.Guizhou Acad Agr Sci, Guizhou Fruit Inst, Guiyang 550006, Peoples R China
2.Sinphar Tian Li Pharmaceut Co Ltd, R&D Ctr, Hangzhou 311100, Peoples R China
3.Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 550025, Peoples R China
4.Guizhou Univ, Ctr R&D Fine Chem, Guiyang 550025, Peoples R China
关键词： Synthesis;Asymmetric curcumin analogs;Quinazoline derivatives of curcumin;Antitumor activity;MGC-803;Apoptosis
期刊名称：CHEMISTRY CENTRAL JOURNAL （ 影响因子：4.215； 五年影响因子：3.836 ）
ISSN： 1752-153X
年卷期： 2017 年 11 卷
页码：
收录情况： SCI
摘要： Background: Cancer is one of the leading causes of death and only second to heart diseases. Recently, preclinical studies have demonstrated that curcumin had a number of anticancer properties. Thus, we planned to synthesize a series of curcumin analogs to assess their antiproliferation efficacy. Results: A series of (1E,4E)-1-aryl-5-(2-((quinazolin-4-yl) oxy)phenyl)-1,4-pentadien-3-one derivatives (curcumin analogs) were synthesized and characterized by IR, NMR, and elemental analysis techniques. All of the prepared compounds were screened for antitumor activities against MGC-803, PC3, and Bcap-37 cancer cell lines. A significant inhibition for cancer cells were observed with compound 5f and also less toxic on NIH3T3 normal cells. The mechanism of cell death induced by compound 5f was further investigated by acridine orange/ethidium bromide staining, Hoechst 33,258 staining, TUNEL assay, and flow cytometry cytometry, which revealed that the compound can induce cell apoptosis in MGC-803 cells. Conclusions: This study suggests that most of the derivatives could inhibit the growth of human cancer cell lines. In addition, compound 5f could induce apoptosis of cancer cells, and it should be subjected to further investigation as a potential anticancer drug candidate.
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