新型N-（胍基）苯磺酰胺的合成及抗乳腺癌评估
Synthesis and anti-breast cancer evaluation of novel N-(guanidinyl)benzenesulfonamides.
作者信息
Ghorab Mostafa M, El-Gazzar Marwa G, Alsaid Mansour S
机构信息
Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo 11371, Egypt.
出版信息
Int J Mol Sci. 2014 Apr 1;15(4):5582-95. doi: 10.3390/ijms15045582.
A series of 4-(substituted)-N-(guanidinyl)benzenesulfonamides bearing biologically active pyrazole, pyrimidine and pyridine moieties were prepared and evaluated for their anticancer activity against human tumor breast cell line (MCF7). These sulfonamides showed promising activity with IC50 values ranging from 49.5 to 70.2 μM. The structure-activity relationship of the synthesized compounds was studied. Interestingly, it was found that the most potent compounds in this study were the corresponding 2-cyanoacrylate 3, 3-oxobutanoate 4, pyrazole 6, pyridine 9 and pyrazole 13. Compounds 7 and 8 are nearly as active as Doxorubicin as reference drug with (IC50 values=70.2, 68.1 μM), while compounds 5, 10 and 11 exhibited a moderate activity.
制备了一系列带有具有生物活性的吡唑、嘧啶和吡啶部分的4-（取代）-N-（胍基）苯磺酰胺，并评估了它们对人肿瘤乳腺癌细胞系（MCF7）的抗癌活性。这些磺酰胺显示出有前景的活性，IC50值范围为49.5至70.2μM。研究了合成化合物的构效关系。有趣的是，发现本研究中最有效的化合物是相应的2-氰基丙烯酸酯3、3-氧代丁酸酯4、吡唑6、吡啶9和吡唑13。化合物7和8的活性几乎与作为参考药物的阿霉素相同（IC50值 = 70.2、68.1μM），而化合物5、10和11表现出中等活性。
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