期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 31, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2020.115953
关键词
Androgen receptor; Novel thiohydantoin derivatives; Androgen receptor antagonists; Prostate cancer
资金
- National Natural Science Foundation of China [82073684]
Prostate cancer is the most common malignancy in men worldwide. In this study, novel thiohydantoin derivatives of enzalutamide were designed and synthesized, with compound 31c identified as a more potent AR antagonist than enzalutamide. The data suggest that 31c could be a promising lead compound for the treatment of prostate cancer.
Prostate cancer (PC) is the most common malignancy in men worldwide. Here, two series of novel thiohydantoin derivatives of enzalutamide as potent androgen receptor (AR) antagonists were designed and synthesized. Among them, compound 31c was identified as an AR antagonist which is 2.3-fold more potent than enzalutamide. Molecular docking studies were performed to explain the improved potency of 31c at AR. In cell proliferation assays, 31c exhibited similar anti-proliferative activities with enzalutamide against hormone sensitive LNCaP cells and AR-overexpressing LNCaP/AR cells. These data indicate that 31c can be a good lead compound for further structure optimization for the treatment of prostate cancer.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据