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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Antitumor activities of biscoumarin and dihydropyran derivatives
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Antitumor activities of biscoumarin and dihydropyran derivatives

机译：双香豆素和二氢吡喃衍生物的抗肿瘤活性

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摘要

Rising worldwide cancer incidence and resistance to current anti-cancer drugs necessitate the need for new pharmaceutical compounds and drug delivery system. Two novel series of biscoumarin (1-4) and dihydropyran (5-16) derivatives were synthesized via a one-pot multicomponent condensation reaction and evaluated for their antitumor activity in vitro. The X-ray crystal structure analysis of four representative compounds 2, 7, 10 and 13 confirmed the structures of these compounds. Compounds 1-4 showed the most potent antitumor activity among the total 16 derivatives. More interestingly, preliminary mechanism studies revealed that the most potent compound 4 induced apoptosis and arrested the cell cycle at the S phase in HUTU80 cells. Additionally, the increased accumulation of HUTU80 cells in the sub G1 peak further pointed to the occurence of the cell apoptosis. The selectivity index analysis demonstrated that all the biscoumarin compounds (SI = 3.1-7.5) possess higher selectivity towards intestinal epithelial adenocarcinoma cell line (HuTu80) than positive control drug carboplatin (SI = 1.6-1.8). The biscoumarin compounds also showed no obvious acute toxicity on mice. (C) 2016 Elsevier Ltd. All rights reserved.
机译：全球范围内癌症发病率的上升和对当前抗癌药的耐药性使得需要新的药物化合物和药物递送系统。通过一锅多组分缩合反应合成了两个新颖的双香豆素（1-4）和二氢吡喃（5-16）衍生物，并评估了它们的体外抗肿瘤活性。四种代表性化合物2、7、10和13的X射线晶体结构分析证实了这些化合物的结构。在总共16种衍生物中，化合物1-4显示出最有效的抗肿瘤活性。更有趣的是，初步的机制研究表明，最有效的化合物4诱导了HUTU80细胞的凋亡并使其细胞周期停滞在S期。此外，HUTU80细胞在sub G1峰中积累的增加进一步表明细胞凋亡的发生。选择性指数分析表明，所有双香豆素化合物（SI = 3.1-7.5）对肠上皮腺癌细胞系（HuTu80）的选择性都比阳性对照药物卡铂（SI = 1.6-1.8）高。双香豆素类化合物对小鼠也没有明显的急性毒性。 （C）2016 Elsevier Ltd.保留所有权利。

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