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一个巴掌拍不响:具有潜在抗肿瘤活性的含两个氧化还原活性中心的细胞毒性醌类化合物的合成。

It takes two to tango: synthesis of cytotoxic quinones containing two redox active centers with potential antitumor activity.

作者信息

Lima Daisy J B, Almeida Renata G, Jardim Guilherme A M, Barbosa Breno P A, Santos Augusto C C, Valença Wagner O, Scheide Marcos R, Gatto Claudia C, de Carvalho Guilherme G C, Costa Pedro M S, Pessoa Claudia, Pereira Cynthia L M, Jacob Claus, Braga Antonio L, da Silva Júnior Eufrânio N

机构信息

Department of Physiology and Pharmacology, Federal University of Ceará Fortaleza 60430-270 Ceará Brazil.

Division of Bioorganic Chemistry, School of Pharmacy, University of Saarland 66123 Saarbruecken Germany.

出版信息

RSC Med Chem. 2021 Aug 12;12(10):1709-1721. doi: 10.1039/d1md00168j. eCollection 2021 Oct 20.

Abstract

We report the synthesis of 47 new quinone-based derivatives click chemistry and their subsequent evaluation against cancer cell lines and the control L929 murine fibroblast cell line. These compounds combine two redox centers, such as an -quinone/-quinone or quinones/selenium with the 1,2,3-triazole nucleus. Several of these compounds present IC values below 0.5 μM in cancer cell lines with significantly lower cytotoxicity in the control cell line L929 and good selectivity index. Hence, our study confirms the use of a complete and very diverse range of quinone compounds with potential application against certain cancer cell lines.

摘要

我们报告了47种基于醌的新型衍生物的合成,通过点击化学方法合成,并随后对癌细胞系和对照L929小鼠成纤维细胞系进行评估。这些化合物结合了两个氧化还原中心,如对醌/对醌或醌/硒与1,2,3-三唑核。其中几种化合物在癌细胞系中的IC值低于0.5μM,在对照细胞系L929中的细胞毒性显著较低,且具有良好的选择性指数。因此,我们的研究证实了使用一系列完整且非常多样的醌类化合物,它们具有针对某些癌细胞系的潜在应用价值。

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