表皮生长因子受体
表皮生长因子受体抑制剂
化学
IC50型
A549电池
对接(动物)
体外
蛋白质数据库
药理学
受体
生长抑制
计算生物学
癌症研究
生物化学
生物
医学
护理部
作者
Hong Yan,Hongjun Wang,Na Tian,Dongchen Chu
出处
期刊:Letters in Drug Design & Discovery
[Bentham Science]
日期:2024-03-01
卷期号:21 (3): 552-558
标识
DOI:10.2174/1570180819666220928151144
摘要
Background: Epidermal growth factor receptor (EGFR) is a validated and therapeutically amenable target, and inhibition of the EGFR signaling pathway has emerged as an attractive target for cancer therapy. Methods: The present work was designed to synthesize and evaluate the antiproliferative activity of a novel series of 3,9-dioxatetraasteranes as potential inhibitors of EGFR. All target compounds were evaluated for antiproliferative activity in vitro against A549 and HepG2 cell lines. Results: Among the target compounds, compound B13 displayed the most potent antiproliferative activity against A549 with IC50 = 4.31 μM and HepG2 with IC50 = 6.92 μM. In addition, a molecular docking study was performed to investigate the binding mode and binding capacity with EGFR (PDB code: 1M17). Conclusion: The results indicated that 3,9-dioxatetraasteranes may be promising potential EGFR inhibitors.
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