| Autor: |
Ji Zhou, Li-Zhen Yu, Ya-Li Fan, Ci-Hao Guo, Xiao-Mei Lv, Zhi-Yin Zhou, Hui-Dan Huang, Dong-Dong Miao, Sheng-Peng Zhang, Xin-Yu Li, Ping-Ping Zhao, Xiao-Ping Liu, Wei-Hua Hu, Chao Zhang |
| Rok vydání: |
2023 |
| Předmět: |
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| Zdroj: |
European Journal of Medicinal Chemistry. 245:114860 |
| ISSN: |
0223-5234 |
| DOI: |
10.1016/j.ejmech.2022.114860 |
| Popis: |
In order to take advantage of both immunotherapeutic and metabolic antitumor agents, novel dual indoleamine 2,3- dioxygenase 1 (IDO1) and thioredoxin reductase 1 (TrxR1) inhibitors were designed. Thioredoxin reductase 1 (TrxR1) is a main ROS modulator within CRC cells. Indoleamine 2,3-dioxygenase (IDO1) is crucial controller for tryptophan (Trp) metabolism that is also important for CRC immunotherapy. Herein, ten compounds 12a-j containing hydroxyamidine scaffold were designed, synthesized and evaluated for inhibitory activities against IDO1/TrxR1 enzyme and CRC cells. Among these compounds, the most active compound 12d (ZC0109) showed excellent and balanced activity against both IDO1 (IC |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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Full Text from ScienceDirect