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Andrzej Zieba¹, Dominika Pindjakova², Malgorzata Latocha³

¹Department of Organic Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Jagiellonska 4, 41-200 Sosnowiec, Poland.

Molecules (Basel, Switzerland)

|September 14, 2024

概括

新的林硫胺衍生物被合成并测试了抗癌和抗菌活性. 化合物3c对癌细胞系和耐药细菌具有显著的有效性,对正常细胞没有毒性.

科学领域:

药用化学医学化学
有机合成有机合成
药理学药理学是指药理学的学科.

背景情况:

昆衍生物因其多样化的生物活性而闻名.
硫胺基支架在各种治疗剂中普遍存在.
混合分子结合oline和triazole系统为新药发现提供了潜在的潜力.

研究的目的:

为了合成8-基和8-甲氧基诺林-5-硫胺的新型乙衍生物.
创建含有林和1,2,3-三醇部分的混合系统.
评估合成化合物的抗癌和抗微生物潜力.

主要方法:

通过硫基化物与氨基衍生物的反应合成氨酸胺 quinoline衍生物.
通过与有机亚酸盐的反应,制备oline-triazole混合系统.
使用NMR光谱和HR-MS进行结构性表征.
在体外对人类黑色素瘤,乳腺癌和肺癌细胞系进行抗癌活性测试.
对参考和多药耐药细菌菌株进行抗菌活性评估.
对正常人皮肤纤维细胞的细胞毒性评估.

主要成果:

8-基-5-硫胺 (3a-f) 的乙衍生物表现出显著的生物活性.
化合物3c (8-hydroxy-N-methyl-N-(prop-2-yn-1-yl) quinoline-5-sulfonamide) 显示出最高的抗癌和抗菌疗效.
化合物3c的抗癌活性与西斯普拉丁和多克索鲁比辛可比,其抗菌活性与西林和西普罗夫洛克萨相美.
化合物3c对正常人皮肤纤维细胞没有毒性,直至100μM.
关键蛋白质 (H3,P53,P21) 和参与癌症进展的基因 (BCL-2,BAX) 的复合3c调节表达.
鉴定出氨酸核心第8位的非替代基组对生物活性至关重要.

结论:

新型林硫胺衍生物具有有前途的抗癌和抗菌特性.
化合物3c是进一步开发抗癌和耐药细菌感染的有力主导候选物.
对于观察到的生物活动来说,8-基诺林支架是必不可少的.
合成的化合物代表了对潜在治疗剂的武器库的宝贵补充.

关键词:

一,二,三三醇是什么 8-氧诺林的使用方法乙烯衍生物中的乙烯衍生物.它具有抗菌活性,具有抗菌活性.它具有抗癌活性,具有抗癌活性.细胞毒性细胞毒性综合合成是一种合成.

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