在寻找基于Indole Pharmacophore的表皮生长因子受体 (EGFR) 抑制剂的最新发展
Shweta Mishra1, Adarsh Sahu2,3, Avneet Kaur1
1SGT College of Pharmacy, SGT University, Gurugram, Haryana, 122505, India.
Current topics in medicinal chemistry
|November 1, 2023
概括
新的以醇为基础的化合物显示出作为表皮生长因子受体 (EGFR) 抑制剂用于癌症治疗的前景. 本综述探讨了它们的结构-活性关系以及在各种癌症中克服药物耐药性的潜力.
科学领域:
- 在瘤学瘤学.
- 药用化学 医学化学
- 分子生物学分子生物学
背景情况:
- 皮表皮生长因子受体 (EGFR) 是细胞信号传递和增殖的关键调节器,与各种癌症有关.
- 向EGFR是一种有效的策略,用于治疗乳腺,肺,宫,质瘤和膀癌.
- 对现有的EGFR抑制剂获得的耐药性需要开发新的治疗药物.
研究的目的:
- 审查以醇为基础的化合物作为表皮生长因子受体的强有力的抑制剂.
- 探索这些抑制剂与EGFR活性位点的结构-活性关系.
- 讨论它们的合成和潜在药物开发的分子对接.
主要方法:
- 文献综述侧重于基于醇的EGFR抑制剂.
- 对已识别的化合物的结构-活性关系 (SAR) 的分析.
- 在基分子对接研究中,以评估与EGFR的结合亲和力.
主要成果:
- 基于indole的支架显示出作为EGFR抑制剂的巨大潜力.
- 特定的结构修改与增强的结合和抑制活性相关.
- 分子对接研究预测了与EGFR活性部位的有利相互作用.
结论:
- 基于英多尔的抑制剂是克服EGFR抑制剂耐药性的有前途的化合物类别.
- 对SAR和合成的进一步研究可以导致新的抗癌药物.
- 用新药向EGFR仍然是癌症治疗中的关键策略.
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