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设计,合成和生物评价的印度尔-2-碳胺作为潜在的多目标抗增殖剂

Lamya H Al-Wahaibi¹, Anber F Mohammed², Mostafa H Abdelrahman³

¹Department of Chemistry, College of Sciences, Princess Nourah bint Abdulrahman University, Riyadh 11564, Saudi Arabia.

Pharmaceuticals (Basel, Switzerland)

|July 29, 2023

概括

新的英多尔衍生物显示出对癌症细胞系的强有力的抗增殖作用. 化合物Va对EGFR,BRAF和VEGFR-2具有显著的抑制活性,这表明其具有治疗潜力.

科学领域:

药用化学医学化学
分子生物学分子生物学
计算化学计算化学

背景情况:

癌症仍然是全球主要的死亡原因,需要开发新的治疗药物.
抑制EGFR,BRAF和VEGFR-2等关键信号通路的向疗法在癌症治疗中表现有前途.

研究的目的:

设计和合成新的基于醇的衍生物.
评估这些化合物对癌症细胞系的抗增殖活性.
研究它们对EGFR,BRAF^V600E和VEGFR-2的抑制潜力,并通过in silico对接探索它们的结合模式.

主要方法:

基于醇的衍生物的化学合成 (IV,Va-I).
对于EGFR,BRAFV600E和VEGFR-2.的体外抗增殖试验 (GI₅₀) 和酶抑制试验 (IC₅₀) 进行.
在基分子对接研究中.

主要成果:

化合物Va-i显示出显著的抗增殖活性 (GI₅₀: 2686 nM).
化合物Va对EGFR (IC₅₀ = 71nM) 和BRAF^V600E (IC₅₀范围:77107nM) 显示出强大的抑制作用.
在基对接提供了关于化合物与酶的结合相互作用的见解.

结论:

合成的醇衍生物,特别是化合物Va,表现出有前途的抗癌特性.
化合物Va对关键瘤原体标具有显著的抑制活性,因此需要对癌症治疗进行进一步的研究.
分子对接研究支持这些化合物作为EGFR,BRAF^V600E和VEGFR-2的抑制剂的潜力.

关键词:

这是一种抗增殖药物.灭症 (apoptosis) 是一种死亡的过程.停靠的对接方式印度尔 (Indole) 是一种制剂.激酶激酶是一种激素.

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