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![]() ![]() |
刊名 | ARCHIV DER PHARMAZIE
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出版日期 | 2018-11 |
卷号 | 351期号:11 |
关键词 | androgen receptor antagonist enzalutamide pentafluorosulfanyl |
ISSN号 | 0365-6233 |
DOI | 10.1002/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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