Ghorab M M, Ragab F A, Heiba H I, El-Gazzar M G, El-Gazzar M G
Department of Drug Radiation Research, National Center for Radiation Research and Technology, Atomic Energy Authority, Cairo, Egypt.
Arzneimittelforschung. 2012 Jan;62(1):46-52. doi: 10.1055/s-0031-1295496. Epub 2012 Jan 10.
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.
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。
