L. Beliyaiah, A. Dilkalal, Vinaya, U. Basavaiah, S. Parkin, R. J. Butcher, H. S. Yathirajan, Y. B. Basavaraju
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引用次数: 0
摘要
本研究通过各种磺酰氯与 2-(哌嗪-1-基)乙胺的辛斯伯格反应合成了二磺酰胺类哌嗪衍生物,并对其细胞增殖活性进行了评估。所有合成化合物均通过 1H、13C NMR、质谱和 X 射线晶体学技术进行了表征。X 射线衍射研究表明,每个结构中都存在中心的哌嗪环和两个末端由磺酰胺连接的取代磺酰基苯基环。在人颊粘膜口腔成纤维细胞原代细胞系上测定了合成化合物的细胞增殖活性。在合成的化合物中,4-硝基-N-(2-{4-[(4-硝基苯基)磺酰基]哌嗪-1-基}乙基)苯磺酰胺、4-(三氟甲基)-N-[2-(4-[4-(三氟甲基)苯基]磺酰基}哌嗪-1-基)乙基]苯磺酰胺和 2-硝基-N-(2-{4-[(2-硝基苯基)磺酰基]哌嗪-1-基}乙基)苯磺酰胺对测试的细胞株具有潜在的活性。
Disulfonamide Piperazine Derivatives: Synthesis, Characterization, Crystal Structures Studies, and Evaluation of Cell Proliferation Activity
In the present study, disulfonamides piperazine derivatives were synthesized by Hinsberg reaction of various sulfonyl chlorides with 2-(piperazin-1-yl)ethanamine and evaluation their cell proliferation activity. All the synthesized compounds were characterized by 1H, 13C NMR, mass spectrometry and X-ray crystallographic techniques. X-ray diffraction studies revealed that the central piperazine ring and two terminal substituted sulfonyl phenyl rings joined by sulfonamide linkage are present in every structure. The cell proliferation activity of synthesized compounds was measured on human buccal mucosa oral fibroblast primary cell lines. Among the synthesized compounds, 4-nitro-N-(2-{4-[(4-nitrophenyl)sulfonyl]piperazin-1-yl}ethyl)benzenesulfonamide, 4-(trifluoromethyl)-N-[2-(4-[4-(trifluoromethyl)phenyl]sulfonyl}piperazin-1-yl)ethyl]benzenesulfonamide and 2-nitro-N-(2-{4-[(2-nitrophenyl)sulfonyl]piperazin-1-yl}ethyl)benzenesulfonamide showed potential activity against tested cell lines.
期刊介绍:
Russian Journal of General Chemistry is a journal that covers many problems that are of general interest to the whole community of chemists. The journal is the successor to Russia’s first chemical journal, Zhurnal Russkogo Khimicheskogo Obshchestva (Journal of the Russian Chemical Society ) founded in 1869 to cover all aspects of chemistry. Now the journal is focused on the interdisciplinary areas of chemistry (organometallics, organometalloids, organoinorganic complexes, mechanochemistry, nanochemistry, etc.), new achievements and long-term results in the field. The journal publishes reviews, current scientific papers, letters to the editor, and discussion papers.