| Autor: |
Siyu He, Yang Liu, Xianglin Chu, Qi Li, Weiping Lyu, Yijun Liu, Shuaishuai Xing, Feng Feng, Wenyuan Liu, Qinglong Guo, Li Zhao, Haopeng Sun |
| Rok vydání: |
2022 |
| Předmět: |
|
| Zdroj: |
ACS medicinal chemistry letters. 13(8) |
| ISSN: |
1948-5875 |
| Popis: |
As a crucial target which is overexpressed in a variety of cancers, aldo-keto reductase 1C3 (AKR1C3) confers chemotherapeutic resistance to many clinical agents. However, a limited number of AKR1C3-selective inhibitors are applied clinically, which indicates the importance of identifying active compounds. Herein, we report the discovery, synthesis, and evaluation of novel and potent AKR1C3 inhibitors with structural diversity. Molecular dynamics simulations of these active compounds provide reasonable clarification of the interpreted biological data. Moreover, we demonstrate that AKR1C3 inhibitors have the potential to be superior therapeutic agents for re-sensitizing drug-resistant cell lines to chemotherapy, especially the pan-AKR1C inhibitor |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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