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黄酮-1,2,3-三唑杂合体的合成及体外抗癌活性评价。

Synthesis and In Vitro Anticancer Evaluation of Flavone-1,2,3-Triazole Hybrids.

机构信息

Department of Organic Chemistry and Technology, Faculty of Chemical Technology and Biotechnology, Budapest University of Technology and Economics, Műegyetem rkp. 3., H-1111 Budapest, Hungary.

Institute of Pharmacognosy, University of Szeged, Eötvös u. 6., H-6720 Szeged, Hungary.

出版信息

Molecules. 2023 Jan 7;28(2):626. doi: 10.3390/molecules28020626.

Abstract

Hybrid compounds of flavones, namely chrysin and kaempferol, and substituted 1,2,3-triazole derivatives, were synthesized by click reaction of the intermediate -propargyl derivatives. 4-Fluoro- and 4-nitrobenzyl-1,2,3-triazole-containing hybrid molecules were prepared. The mono- and bis-coupled hybrids were investigated on 60 cell lines of 9 common cancer types (NCI60) in vitro as antitumor agents. Some of them proved to have a significant antiproliferative effect.

摘要

黄酮类化合物(如白杨素和山奈酚)与取代的 1,2,3-三唑衍生物的杂合化合物通过中间物炔丙基衍生物的点击反应合成。制备了含有 4-氟和 4-硝基苄基-1,2,3-三唑的杂合分子。作为抗肿瘤药物,对包含单和双偶联的杂合分子在 9 种常见癌症类型的 60 个细胞系(NCI60)中进行了体外研究。其中一些被证明具有显著的抗增殖作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d009/9860848/26ee0bdbac41/molecules-28-00626-g001.jpg

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