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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis of 5-(4-(1H-phenanthro[9,10-d]imidazol-2-yl)benzylidene) thiazolidine-2,4-dione as promising DNA and serum albumin-binding agents and evaluation of antitumor activity
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Synthesis of 5-(4-(1H-phenanthro[9,10-d]imidazol-2-yl)benzylidene) thiazolidine-2,4-dione as promising DNA and serum albumin-binding agents and evaluation of antitumor activity

机译：合成5-（4-（1H-（1H-（1H-（1H-菲拉米咪唑-2-基）苄基那）噻唑烷-2,4-二酮作为有前途的DNA和血清白蛋白结合剂和抗肿瘤活性的评价

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摘要

A series of phenanthro[9,10-d]imidazole/oxazole and acenaphtho[1,2-d]imidazole with different aryl groups at C2-position has been synthesized. These compounds were in vitro evaluated for antitumor activity against a panel of 60 human cancer cell lines. Compound 8 exhibits higher cytotoxicity towards leukemia, colon, melanoma, renal, and breast cancer cell lines than the other evaluated cell panels and low toxicity against normal cell line Hek293. The binding properties of compound 8 with DNA have been investigated with absorption, emission and circular dichroism as well as thermal denaturation experiments which indicate intercalation with base pairs of human and calf thymus DNA. The molecular docking and site-selective binding studies also reveal the predominant intercalation of compound 8 in base pairs of DNA. The interaction between thiazolidine based phenanthrene 8 and serum albumins (HSA and BSA), transport proteins, has also been explored which shows quenching of fluorescence through static mechanism. The thermodynamic parameters, obtained from van't Hoff relationship indicate the prevalence of hydrogen-bonding/hydrophobic interactions for the binding phenomenon. (C) 2019 Elsevier Masson SAS. All rights reserved.
机译：已经合成了一系列菲[9,10-D]咪唑/氧唑和亚替唑[1,2-D]咪唑，在C2位置下具有不同芳基。将这些化合物对抗肿瘤活性进行体外，针对60例人癌细胞系的面板进行抗肿瘤活性。化合物8对白血病，结肠，黑素瘤，肾病和乳腺癌细胞系具有比其他评估的细胞面板和对正常细胞系HEK293的低毒性的细胞毒性更高的细胞毒性。已经研究了具有DNA的化合物8的结合特性，并进行了吸收，发射和圆形二色性以及热变性实验，表明与碱基对的人和小牛胸腺DNA嵌入。分子对接和位点选择性结合研究还揭示了化合物8在碱基对DNA中的主要插入。还探讨了噻唑烷基的菲苯乙烯8和血清蛋白（HSA和BSA），运输蛋白质之间的相互作用，其通过静态机构显示荧光的猝灭。从Van't Hoff关系获得的热力学参数表示结合现象的氢键/疏水相互作用的患病率。 （c）2019年Elsevier Masson SAS。版权所有。

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