(1E,4E)-1-芳基-5-(2-((喹唑啉-4-基)氧基)苯基)-1,4-戊二烯-3-酮衍生物的合成和体外抗肿瘤活性。,BMC Chemistry

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(1E,4E)-1-芳基-5-(2-((喹唑啉-4-基)氧基)苯基)-1,4-戊二烯-3-酮衍生物的合成和体外抗肿瘤活性。
BMC Chemistry ( IF 4.3 ) Pub Date : 2017-03-15 , DOI: 10.1186/s13065-017-0253-9
Hui Luo _{1,

2,

3} , Shengjie Yang _{2,

3,

4} , Da Hong ₄ , Wei Xue _{2,

3} , Pu Xie ₁

Affiliation

背景技术癌症是导致死亡的主要原因之一，仅次于心脏病。最近，临床前研究表明姜黄素具有多种抗癌特性。因此，我们计划合成一系列姜黄素类似物来评估其抗增殖功效。结果合成并表征了一系列(1E,4E)-1-芳基-5-(2-((喹唑啉-4-基)氧基)苯基)-1,4-戊二烯-3-酮衍生物(姜黄素类似物)通过红外、核磁共振和元素分析技术。筛选所有制备的化合物针对 MGC-803、PC3 和 Bcap-37 癌细胞系的抗肿瘤活性。观察到化合物 5f 对癌细胞有显着的抑制作用，并且对 NIH3T3 正常细胞的毒性也较小。通过吖啶橙/溴化乙锭染色、Hoechst 33,258染色、TUNEL实验和流式细胞仪进一步研究了化合物5f诱导细胞死亡的机制，结果表明该化合物可以诱导MGC-803细胞凋亡。结论这项研究表明大多数衍生物可以抑制人类癌细胞系的生长。此外，化合物5f可诱导癌细胞凋亡，应作为潜在的抗癌候选药物进行进一步研究。

"点击查看英文标题和摘要"

Synthesis and in vitro antitumor activity of (1E,4E)-1-aryl-5-(2-((quinazolin-4-yl)oxy)phenyl)-1,4-pentadien-3-one derivatives.

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.

更新日期：2019-11-01

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