Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer
文献类型：期刊论文
| 作者 | Wang, Ao1,2; Wang, Yawan3; Meng, Xin2; Yang, Yushe1,2,3
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2021-02-01 |
| 卷号 | 31页码:13 |
| 关键词 | Androgen receptor Novel thiohydantoin derivatives Androgen receptor antagonists Prostate cancer |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2020.115953 |
| 通讯作者 | Yang, Yushe(ysyang@simm.ac.cn) |
| 英文摘要 | 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. |
| 资助项目 | National Natural Science Foundation of China[82073684] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000616108800010 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/295713]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Yang, Yushe |
| 作者单位 | 1.Univ Chinese Acad Sci, Sch Pharm, 19A Yuquan Rd, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Ave, Nanjing 210023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Wang, Ao,Wang, Yawan,Meng, Xin,et al. Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2021,31:13. |
| APA | Wang, Ao,Wang, Yawan,Meng, Xin,&Yang, Yushe.(2021).Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer.BIOORGANIC & MEDICINAL CHEMISTRY,31,13. |
| MLA | Wang, Ao,et al."Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer".BIOORGANIC & MEDICINAL CHEMISTRY 31(2021):13. |
入库方式： OAI收割
来源：上海药物研究所
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