Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer

doi:10.1016/j.bmc.2020.115953

	Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer
	Wang, Ao 2,3; Wang, Yawan 1; Meng, Xin 3; Yang, Yushe 1,2,3
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	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
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000616108800010
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/295713]
专题	中国科学院上海药物研究所
通讯作者	Yang, Yushe
作者单位	1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Ave, Nanjing 210023, Peoples R China 2.Univ Chinese Acad Sci, Sch Pharm, 19A Yuquan Rd, Beijing 100049, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, 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.