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Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity

文献类型：期刊论文

作者Ma, Longjun2,3; Zhou, Yan1; Yang, Dehua1; Wang, Ming-Wei1; Lu, Wei2; Jin, Jiyu2
刊名MOLECULES
出版日期2022-09-01
卷号27期号:18页码:22
关键词androgen receptor antagonist enzalutamide hydantoin analogs antiproliferative
DOI10.3390/molecules27185867
通讯作者Wang, Ming-Wei(mwwang@simm.ac.cn) ; Lu, Wei(wlu@chem.ecnu.edu.cn) ; Jin, Jiyu(jyjin@chem.ecnu.edu.cn)
英文摘要Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities. Among them, compounds 6a/6c/7g/19a/19b exhibited excellent androgen receptor antagonistic activity, which was consistent with or even superior to enzalutamide. In addition, compounds 19a and 19b exhibited better antiproliferative activity than enzalutamide in prostate cancer cells. The results show that compound 19a has great potential as a new AR antagonist.
WOS关键词RESISTANT PROSTATE-CANCER ; ANTIANDROGEN ; MDV3100 ; DESIGN
资助项目Personalized Medicines-Molecular Signaturebased Drug Discovery and Development Strategic Priority Research Program of Chinese Academy of Sciences[XDA12020347] ; Personalized Medicines-Molecular Signaturebased Drug Discovery and Development Strategic Priority Research Program of Chinese Academy of Sciences[XDA12040308] ; Thousand Talents Program in China ; Shanghai Science and Technology Council[16DZ2280100]
WOS研究方向Biochemistry & Molecular Biology ; Chemistry
语种英语
WOS记录号WOS:000856961200001
出版者MDPI
源URL[http://119.78.100.183/handle/2S10ELR8/302474]  
专题中国科学院上海药物研究所
通讯作者Wang, Ming-Wei; Lu, Wei; Jin, Jiyu
作者单位1.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 189 Guo Shou Jing Rd, Shanghai 200031, Peoples R China
2.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Sch Chem & Mol Engn, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China
3.Lanzhou Jiaotong Univ, Sch Chem & Chem Engn, Dept Appl Chem, 88 Anning West Rd, Lanzhou 730070, Peoples R China
推荐引用方式
GB/T 7714		 Ma, Longjun,Zhou, Yan,Yang, Dehua,et al. Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity[J]. MOLECULES,2022,27(18):22.
APA Ma, Longjun,Zhou, Yan,Yang, Dehua,Wang, Ming-Wei,Lu, Wei,&Jin, Jiyu.(2022).Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity.MOLECULES,27(18),22.
MLA Ma, Longjun,et al."Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity".MOLECULES 27.18(2022):22.

入库方式： OAI收割

来源：上海药物研究所

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