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Synthesis of androgen receptor antagonists containing a pentafluorosulfanyl (SF5) moiety

文献类型：期刊论文

作者Jin, Jiyu3; Zhou, Yan1,2; Yang, Dehua1,2; Zhang, Qiumeng3; Wang, Ming-Wei1,2; Lu, Wei3
刊名ARCHIV DER PHARMAZIE
出版日期2018-11
卷号351期号:11
关键词androgen receptor antagonist enzalutamide pentafluorosulfanyl
ISSN号0365-6233
DOI10.1002/ardp.201800175
文献子类Article
英文摘要A novel scaffold of pentafluorosulfanyl (SF5)-containing enzalutamide analogues was discovered for potent androgen receptor (AR) antagonists through rational drug design. Several compounds showed good biological profiles in AR binding. Of the derivatives studied, compound 8a had potent AR antagonist activity (IC50 = 7.1 +/- 1.0 mu M) and high efficacy (104.5 +/- 12.8%). It exhibited an inhibitory effect comparable to that of enzalutamide (inhibition = 66.0 and 77.9%, respectively) in a prostate cancer cell line. The results point to the potential of using this scaffold to develop new AR antagonists.
WOS关键词RESISTANT PROSTATE-CANCER ; BIOLOGICAL-ACTIVITY ; PENTAFLUORIDES ; ANTIANDROGEN ; ANALOGS
资助项目Chinese Academy of Sciences[XDA12020347] ; Chinese Academy of Sciences[XDA12040308] ; Thousand Talents Program in China[00000000] ; Shanghai Science and Technology Council[16DZ2280100]
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000449673500005
出版者WILEY-V C H VERLAG GMBH
源URL[http://119.78.100.183/handle/2S10ELR8/279515]  
专题国家新药筛选中心
通讯作者Wang, Ming-Wei; Lu, Wei
作者单位1.Chinese Acad Sci, Natl Ctr Drug Screening, 189 Guo Shou Jing Rd, Shanghai 201203, Peoples R China;
2.Chinese Acad Sci, Shanghai Inst Materia Med, CAS Key Lab Receptor Res, 189 Guo Shou Jing Rd, Shanghai 201203, Peoples R China
3.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, 3663 North Zhongshan Rd, Shanghai 200062, Peoples R China;
推荐引用方式
GB/T 7714		 Jin, Jiyu,Zhou, Yan,Yang, Dehua,et al. Synthesis of androgen receptor antagonists containing a pentafluorosulfanyl (SF5) moiety[J]. ARCHIV DER PHARMAZIE,2018,351(11).
APA Jin, Jiyu,Zhou, Yan,Yang, Dehua,Zhang, Qiumeng,Wang, Ming-Wei,&Lu, Wei.(2018).Synthesis of androgen receptor antagonists containing a pentafluorosulfanyl (SF5) moiety.ARCHIV DER PHARMAZIE,351(11).
MLA Jin, Jiyu,et al."Synthesis of androgen receptor antagonists containing a pentafluorosulfanyl (SF5) moiety".ARCHIV DER PHARMAZIE 351.11(2018).

入库方式： OAI收割

来源：上海药物研究所

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