Novel indoline-2,3-dione derivatives as inhibitors of aminopeptidase N (APN) |
| |
Authors: | Kang Jin Xiaopan Zhang Chunhua Ma Yingying Xu Yumei Yuan Wenfang Xu |
| |
Affiliation: | Department of Medicinal Chemistry, School of Pharmacy, Shandong University, 44, West Culture Road, Jinan, Shandong 250012, China |
| |
Abstract: | Aminopeptidase N (APN/CD13), as a zinc-containing ectoenzyme, plays a critical role in the process of tumor angiogenesis, invasion and metastasis. Through the docking-based virtual screening of chemical databases and the further activity assay, we discovered that compound 10c exhibits potent and selective inhibitory ability towards APN. In addition, a series of indoline-2,3-dione derivates have been designed and synthesized as APN inhibitors. The results of preliminary activity evaluation showed that compound 12a (IC50 = 0.074 ± 0.0026 μM) exhibited the best inhibitory activity against APN, which could be used for further anticancer agent research. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|