Several N4-substituted aminobenzenesulfonamides derivatives have been synthesized and structural analyses have been carried out using FT-IR, UV-Vis, 1H and 13C NMR, LC-MS-MS and elemental analyses. Photoluminescence and physicochemical properties have also been conducted. Two 4-aminobenzenesulfonamides have been treated with 2-bromopropionyl bromide in pyridine to give their respective bromo substituted aminobenzenesulfonamides as intermediates. Subsequent reactions with morpholino-, thiomorpholino- and piperazine amines have yielded novel aminobenzenesulfonamide derivatives. As it is well known that CA IX and CA XII enzymes play an active role in attacking various cancerous conditions, studies presented in this study target these enzymes with in vitro cytotoxicity studies being performed on the compounds synthesized. The target compounds have been found to be active against some cancerous cells, with mimimal effects on normal cells. The physicochemical data reveal interesting synergistic effects controlling cytotoxicities, where the lipophilicity and polarity combinations play important roles on the eventual observed cytotoxicities. Further, the electronegativity and availability of the electrons of the heteroatoms of the synthesized compounds appear to have an effect on cancer cell cytotoxicities.

中文翻译：

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一些新型N4取代氨基苯磺酰胺的合成、表征、细胞毒性评价和理化性质

已经合成了几种 N4 取代的氨基苯磺酰胺衍生物，并使用 FT-IR、UV-Vis、1H 和 13C NMR、LC-MS-MS 和元素分析进行​​了结构分析。还进行了光致发光和物理化学性质。两种 4-氨基苯磺酰胺已在吡啶中用 2-溴丙酰溴处理，得到它们各自的溴取代氨基苯磺酰胺作为中间体。随后与吗啉、硫代吗啉和哌嗪胺的反应产生了新的氨基苯磺酰胺衍生物。众所周知，CA IX 和 CA XII 酶在攻击各种癌症状况方面发挥着积极作用，本研究中提出的研究针对这些酶，并对合成的化合物进行了体外细胞毒性研究。已发现目标化合物对某些癌细胞具有活性，对正常细胞的影响最小。物理化学数据揭示了控制细胞毒性的有趣协同效应，其中亲脂性和极性组合对最终观察到的细胞毒性起着重要作用。此外，合成化合物杂原子的电子的电负性和可用性似乎对癌细胞的细胞毒性有影响。