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一些新型N-(喹喔啉-2-基)苯磺酰胺衍生物的合成、体外抗癌筛选及放射增敏评估

Synthesis, in-vitro anticancer screening and radiosensitizing evaluation of some new N-(quinoxalin-2-yl)benzenesulfonamide derivatives.

作者信息

Ghorab M M, Ragab F A, Heiba H I, El-Gazzar M G, El-Gazzar M G

机构信息

Department of Drug Radiation Research, National Center for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt.

出版信息

Arzneimittelforschung. 2012 Jan;62(1):46-52. doi: 10.1055/s-0031-1295496. Epub 2012 Jan 10.

Abstract

The objective of this work is to synthesize and investigate the anticancer activity of a new series of sulfaquinoxaline derivatives by incorporating biologically active moieties (thiourethane, thiazole, imidazole, imidazopyrimidine, imidazopyrimido-pyrimidine, thienopyrimidine, benzopyrimidinone, benzothiazole, thiazole and pyridine moieties). All the newly synthesized compounds were evaluated for their in-vitro anticancer activity against human liver cell line (HEPG2). All the tested compounds showed comparable activity to that of the reference drug 5-fluorouracil (IC50=40 µM), and the most potent compounds were found to be compounds 4 and 17 (IC50=4.29 and 11.27 µM, respectively). On the other hand, the most potent compounds 4 and 17 were evaluated as radiosensitizing agents.

摘要

这项工作的目的是通过引入生物活性部分(硫代氨基甲酸酯、噻唑、咪唑、咪唑并嘧啶、咪唑并嘧啶并嘧啶、噻吩并嘧啶、苯并嘧啶酮、苯并噻唑、噻唑和吡啶部分)来合成并研究一系列新的磺胺喹恶啉衍生物的抗癌活性。对所有新合成的化合物进行了针对人肝癌细胞系(HEPG2)的体外抗癌活性评估。所有测试化合物均显示出与参考药物5-氟尿嘧啶(IC50 = 40 μM)相当的活性,发现最有效的化合物是化合物4和17(IC50分别为4.29和11.27 μM)。另一方面,对最有效的化合物4和17进行了放射增敏剂评估。

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