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Evaluation of Nonel N-(piperidin-4-yl)benzamide Derivatives as Potential Cell Cycle Inhibitors in HepG2 cells

Abstract

肝癌是目前世界上引起致高死亡率的疾病之一。细胞周期紊乱是引起肿瘤细胞增殖失控的主要原因,越来越多的学者致力于研究细胞周期抑制剂。索拉非尼作为一个多靶点广谱抗肿瘤药,近几年来基于其结构改造的化合物层出不穷。因此,本文以索拉非尼为先导化合物,保留其二芳醚结构,将脲基改造成酰胺键,并插入一个亲水基团,设计合成了一系列的索拉非尼类似物——N-(4-哌啶基)-苯甲酰胺类化合物,共合成了45个终产物,合成方法简单易操作,产物易纯化,且收率高。通过初步生物学活性的筛选,我们发现其中部分类似物展现良好的抑制HepG2肿瘤细胞生长的活性,特别是化合物47,不仅对HepG2细胞显示出良好的抑制活性(IC50=0....Hepatocellular carcinoma (HCC) is a commonly occurring cancer that has a high mortality rate every year. Uncontrolled cell growth and proliferation are the main features of cancer and the main mechanisms of which occur by cell cycle disorders. Sorafenib as a broad-spectrum and multi-target anti-tumor drug, more and more sorafenib analogues were synthesized for tumor treament in recent years. There...学位:医学硕士院系专业:药学院_药物化学学号:3232012115309

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