酰胺修饰莪术酚衍生物的设计、合成及抗gbm活性研究。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2025-05-06 DOI:10.1016/j.bmcl.2025.130265

Shiqi Hu , Yuhang Fan , Yumo Zhao, Zhengyang Gao, Jie Lu, Jian Li, Jinlian Wei, Yongqiang Zhang

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引用次数: 0

摘要

通过简单的四步法，设计并合成了一系列酰胺修饰的姜黄酚衍生物。值得注意的是，在氮原子上附着苯基或取代苯基的衍生物具有显著增强的体外抗gbm活性和良好的血脑屏障通透性。其中，含4-氟苯基的13 t对GBM细胞活力的抑制作用表现出最有效的剂量依赖性，为进一步发现抗GBM药物提供了新的先导化合物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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Design, synthesis and anti-GBM activities of amide-modified Curcumol derivatives

A series of amide-modified curcumol derivatives have been designed and synthesized via a simple four-step procedure. Notably, the derivatives with a phenyl or substituted phenyl attaching on the nitrogen atom showed significantly enhanced in vitro anti-GBM activity and excellent BBB permeability. Among them, 13t with a 4-fluorophenyl demonstrated the most potent dose-dependent inhibition of GBM cell viability, providing a novel lead compound for further anti-GBM drug discovery.

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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.