Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors.
发布时间：2025-04-30
点击次数：
- 发布时间：
- 2025-04-30
- 论文名称：
- Expanding the structural diversity of diarylureas as multi-target tyrosine kinase inhibitors.
- 发表刊物：
- Bioorganic & Medicinal Chemistry
- 摘要：
- Recently approved multi-target inhibitors of receptor tyrosine kinases (RTKs) have significantly improved the clinical treatment of cancers. A series of N,N'-diarylureas incorporated with aromatic heterocycle have been designed, synthesized and evaluated as novel multi-target RTK inhibitors. The preliminary biological evaluation indicated that several compounds exhibited comparable potency with Sorafenib. Among them, compound 6f was identified as the most potent multikinase inhibitor of EGFR, KDR and FGFR1 with IC50 values of 14.83nM, 21.57nM, and 28.23nM, respectively. These compounds expanded the structural diversity of diarylureas as RTK inhibitors. The results demonstrated that compound 6f could be served as novel lead compound for further development of multi-target RTK inhibitors.
- 合写作者：
- Yuanyuan Shan, Yalin Dong*
- 是否译文：
- 否
- 发表时间：
- 2016-02-15
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