Department of Bioengineering, Karamanoglu Mehmetbey University, 70200, Karaman, Turkey.
Appl Biochem Biotechnol. 2020 Apr;190(4):1484-1497. doi: 10.1007/s12010-019-03184-x. Epub 2019 Nov 28.
Here, new calixarene sulfonamide analogs were synthesized from the reaction of chlorosulfonated calix[n]arene (n: 4, 6, and 8) with N,N'-dimethylethylenediamine or ethylenediamine for the first time and an excellent calixarene sulfonamide analog showing potent and selective cytotoxic activity on some cancer cell lines were discovered. Cytotoxicity of the prepared calix[n]arene sulfonamide analogs towards both cancer and healthy cell lines was assessed by performing cell growth inhibition assays. In cytotoxicity assay results, it was observed that while sulfonamide analog based calix[4]arene (9) was not affecting the growth of epithelial cell lines (HEK), and it was especially effective on inhibiting the growth of some human cancer cell lines (MCF-7 and MIA PaCa-2). These results highlight that sulfonamide analog-based calix [4] arene (9) can be further studied as a potential anticancer agent.
这里,首次通过氯磺酰化杯[n]芳烃(n:4、6 和 8)与 N,N'-二甲乙二胺或乙二胺的反应合成了新的杯[芳烃]磺酰胺类似物,并发现了一种具有优异的细胞毒性活性的杯芳烃磺酰胺类似物对一些癌细胞系具有选择性。通过进行细胞生长抑制试验来评估所制备的杯[n]芳烃磺酰胺类似物对癌细胞系和正常细胞系的细胞毒性。在细胞毒性试验结果中,观察到磺酰胺类似物为基础的杯[4]芳烃(9)不影响上皮细胞系(HEK)的生长,并且对一些人癌细胞系(MCF-7 和 MIA PaCa-2)的生长具有特别有效的抑制作用。这些结果表明,磺酰胺类似物为基础的杯[4]芳烃(9)可以进一步作为一种潜在的抗癌药物进行研究。