Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo, Egypt; Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, Cairo University, Egypt.
Eur J Med Chem. 2015 Mar 6;92:682-92. doi: 10.1016/j.ejmech.2015.01.036. Epub 2015 Jan 20.
In this study, novel series of sulfonamide derivatives were synthesized starting from 2-cyanoacetyl)hydrazono)ethyl)phenyl)benzenesulfonamide 4a and 2-cyanoacetyl)hydrazono)ethyl)phenyl)-4-methylbenzenesulfonamide 4b. Different biologically active moieties as pyrazol, thiophene, pyridine and pyrimidines were introduced in order to investigate their in-vitro anticancer activity, in addition to a novel series of sulfonamide chalcones were synthesized from the reported 4-acetyl-N-(P-tolyl) benzenesulfonamide 3b. The newly synthesized sulfonamide derivatives were characterized by FT-IR, (1)H NMR, (13)C NMR, mass spectroscopy and elemental analyses and were tested for their in-vitro anticancer activity against human tumor liver cell line (HEPG-2). The most potent compounds in this study were compounds 4a, 4b, 5a, 6a, 6b, 8, 9, 11, 13, 18 and 19 which showed higher activity than doxorubicin with IC50 ranging from 11.0 to 31.8 μM. Additionally, eight compounds among the most potent were evaluated for their ability to enhance the cell killing effect of γ-radiation.
在这项研究中，从 2-氰乙酰基）（肼基）乙基）苯基）苯磺酰胺 4a 和 2-氰乙酰基）（肼基）乙基）苯基）-4-甲基苯磺酰胺 4b 出发，合成了一系列新型磺酰胺衍生物。为了研究它们的体外抗癌活性，引入了不同的生物活性基团，如吡唑、噻吩、吡啶和嘧啶，此外，还从报道的 4-乙酰基-N-（对甲苯基）苯磺酰胺 3b 合成了一系列新型磺酰胺查耳酮。新合成的磺酰胺衍生物通过傅里叶变换红外光谱（FT-IR）、（1）H 核磁共振谱（1H NMR）、（13）C 核磁共振谱（13C NMR）、质谱和元素分析进行了表征，并对其进行了体外抗癌活性测试，针对人肿瘤肝细胞系（HEPG-2）。在这项研究中，最有效的化合物是化合物 4a、4b、5a、6a、6b、8、9、11、13、18 和 19，它们的活性高于阿霉素，IC50 范围为 11.0 至 31.8 μM。此外，在最有效的八种化合物中，评估了它们增强 γ 辐射细胞杀伤效应的能力。
