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作为潜在EGFR抑制剂的奇拉尔1,3,5-氨酸:制药模拟,合成,分子对接,分子动力学模拟和抗癌评估

Saravanakumar Natarajan¹, Latha Ganesapandian^1,2, Pandeeshwaran Santhoshkumar¹

¹Supramolecular and Catalysis Lab, Department of Natural Products Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai, India.

Chemistry & biodiversity

|August 29, 2025

概括

在乳腺癌和肺癌中向表皮生长因子受体 (EGFR) 发出信号. 最强效的化合物显示出显著的细胞毒性,表明EGFR向癌症治疗的前景.

科学领域:

医学化学
癌症学
药物设计

背景情况:

表皮生长因子受体 (EGFR) 信号传递是乳腺癌和肺癌的关键目标.
在癌症治疗中,开发具有提高疗效和选择性的新兴抑制剂至关重要.

研究的目的:

设计和合成作为潜在EGFR抑制剂的性1,3,5-衍生物库.
评估这些化合物对乳腺癌 (MCF-7) 和肺癌 (A549) 细胞系的抗癌活性.

主要方法:

用于支架设计的基于联体的药物设计方法.
优化的合成协议,以化纯-1,3,5-衍生物.
通过MTT试验评估体内抗癌活性;在EGFR- TK ATP结合部位进行分子对接.

主要成果:

系统的结构修改导致了微调的物理化学和ADME特性.
分子对接与体外EGFR抑制活性相关.
(R) - 4 - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - 氨基氨基氨基酸基 (13c) 呈现强烈的细胞毒性 (IC50:在MCF-7中为8.04μM,在A549中为12.24μM).

结论:

基1,3,5-氨酸为开发针对EGFR的新型癌症疗法提供了有前途的支架.
合成的化合物显示出在瘤学中进一步发展的巨大潜力.

关键词:

抑制EGFR的活性奇拉-1,3,5-氨酸常见的药基于连接体的设计

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