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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >Synthesis and pro-apoptotic effects of new sulfonamide derivatives via activating p38/ERK phosphorylation in cancer cells
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Synthesis and pro-apoptotic effects of new sulfonamide derivatives via activating p38/ERK phosphorylation in cancer cells

机译：通过激活癌细胞中的p38 / ERK磷酸化作用合成新的磺酰胺衍生物及其促凋亡作用

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Herein, the compounds bearing sulfonamide fragment such as N-(2-amino-5-benzoylphenyl)-4-nitrobenzene sulfonamide hydrochloride (1), N-(quinolin-8-yl)-4-nitro-benzenesulfonamide hydrochloride (2), N-(pyridine-2-ylmethyl)-4-nitro-benzenesulfonamide hydrochloride (3) were synthesized by the reaction of 3,4-diaminobenzophenone, 8-aminoquinoline or 2-picoylamine and 4-nitrobenzensulfonyl chloride, respectively. The structures of the newly synthesized compounds were elucidated on the basis of elemental and spectral analyses. All the prepared compounds were evaluated for their in vitro anti-cancer activity against various cancer cell lines and to explore the underlying molecular mechanisms involved in this process. In vitro cytotoxic activities of the compounds were screened against human hepatocellular (HepG2), breast (MCF-7) and colon (Colo-205) cancer cell lines by MTT assay, mRNA expression of genes with qPCR and phosphorylation of p38 and ERK1/2 with Western blot. Tested compounds could significantly reduce cell proliferation and induced mRNA expression of pro-apoptotic genes; caspase 3, caspase 8 and caspase 9. Activation of these apoptotic genes probably is mediated by activation of p38.
机译：在此，具有磺酰胺片段的化合物例如N-（2-氨基-5-苯甲酰基苯基）-4-硝基苯磺酰胺盐酸盐（1），N-（喹啉-8-基）-4-硝基苯磺酰胺盐酸盐（2）， N-（吡啶-2-基甲基）-4-硝基-苯磺酰胺盐酸盐（3）分别通过3,4-二氨基二苯甲酮，8-氨基喹啉或2-吡啶胺和4-硝基苯磺酰氯的反应合成。在元素分析和光谱分析的基础上阐明了新合成化合物的结构。评价所有制备的化合物对各种癌细胞的体外抗癌活性，并探索该过程涉及的潜在分子机制。通过MTT分析，qPCR基因的mRNA表达以及p38和ERK1 / 2的磷酸化，筛选了该化合物对人肝细胞（HepG2），乳腺癌（MCF-7）和结肠（Colo-205）癌细胞系的体外细胞毒活性。免疫印迹被测化合物可以显着降低细胞增殖并诱导促凋亡基因的mRNA表达。 caspase 3，caspase 8和caspase9。这些凋亡基因的激活可能是由p38的激活介导的。

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