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合成bis-thiohydantoin衍生物作为一种针对EGFR抑制途径的抗增殖剂

Alaa A Hassan¹, Ashraf A Aly², Mohamed Ramadan³

¹Chemistry Department, Faculty of Science, Organic Division, Minia University, El-Minia, 61519, Minia, Egypt. alaahassan2001@mu.edu.eg.

Molecular diversity

|June 12, 2023

概括

新的EGFR抑制剂被合成并测试了它们的抗增殖作用. 化合物4c显示出强大的EGFR抑制和抗癌活性,显示出进一步药物开发的前景.

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:

表皮生长因子受体 (EGFR) 是癌症治疗的关键标.
开发新的EGFR抑制剂对于克服耐药性至关重要.
尿素衍生物已经显示出作为抗癌剂的潜力.

研究的目的:

为了合成新型的伊米达佐利丁衍生物.
评估它们的EGFR抑制活性和抗增殖作用.
阐明反应机制和结构特征.

主要方法:

伊米达佐利丁化合物的二重选择性合成.
使用NMR,IR,质谱和元素分析进行结构性表征.
单晶X射线结构分析.
在体外EGFR抑制试验和抗增殖试验.
分子对接研究. 分子对接研究.

主要成果:

新型 (R) / (S) -3-替代-1-[2-(5) -3-替代-4-基-5-oxo-4-phenyl-2-thioxoimidazolidin-1-yl]乙烯/基-5-基-5-phenyl-2-thioxoimidazolidin-4-ones的新型 (R) / (S) -3-替代-1-[2-(5) -3-替代-4-基-5-oxo-4-phenyl-2-thioxoimidazolidin-1-yl]乙烯/基-5-基-5-phenyl-2-thioxoimidazolidin-4-ones的新型成功合成.
化合物表现出EGFR抑制活性,IC50值在90至178nm之间.
化合物4c (基,n=3) 显示出最强的EGFR抑制 (IC50 = 90nM) 和抗增殖作用.
对接研究表明,4c化合物与EGFR有很高的亲和力.

结论:

合成的伊米达索利丁衍生物具有显著的EGFR抑制和抗增殖活性.
化合物4c是开发针对EGFR的新型抗癌疗法的有前途的主要候选者.
该研究提供了对结构-活动关系和潜在作用机制的见解.

关键词:

抗扩散药物抗扩散药物循环烯是一种环.停靠的对接方式欧洲农业基金会 (EGFR) 是一个.不同周期的异质环.尿酸的使用方法提奥克索伊米达佐利丁-4-ONE是一种

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