Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs

doi:10.3390/molecules24234227

	Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs
	Shao, Pingxuan 2; Zhou, Yan 1,3; Yang, Dehua 1,3; Wang, Ming-Wei 1,3; Lu, Wei 2; Jin, Jiyu 2
刊名	MOLECULES
	2019-12-01
卷号	24 期号:23 页码:13
关键词	pentafluorosulfanyl aryl propionamide androgen receptor agonist SARMs
DOI	10.3390/molecules24234227
通讯作者	Wang, Ming-Wei(mwwang@simm.ac.cn) ; Jin, Jiyu(jyjin@chem.ecnu.edu.cn)
英文摘要	The pentafluorosulfane (SF5) group, as a more electronegative bioisostere than the trifluoromethyl (CF3) group, has been gaining greater attention and increasingly reported usage in medicinal chemistry. Ostarine is the selective androgen receptor modulators (SARMs) containing a CF3 group in clinical trial III. In this study, 21 ostarine derivatives for replacing the CF3 group with SF5 substituents were synthesized. Some SF5-derivatives showed androgen receptor (AR) agonistic activities in vitro. The results pointed to the potential of using this scaffold to develop new AR agonists.
资助项目	Personalized Medicines-Molecular Signature-based Drug Discovery and Development Strategic Priority Research Program of Chinese Academy of Sciences[XDA12020347] ; Personalized Medicines-Molecular Signature-based Drug Discovery and Development Strategic Priority Research Program of Chinese Academy of Sciences[XDA12040308] ; Thousand Talents Program in China ; [16DZ2280100]
WOS关键词	ANDROGEN RECEPTOR MODULATOR ; PHARMACOKINETICS ; DISCOVERY ; CHEMISTRY ; DESIGN ; SAFETY
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	MDPI
WOS记录号	WOS:000507294400026
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/282521]
专题	中国科学院上海药物研究所
通讯作者	Wang, Ming-Wei; Jin, Jiyu
作者单位	1.Chinese Acad Sci, Natl Ctr Drug Screening, 189 Guo Shou Jing Rd, Shanghai 200062, Peoples R China 2.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 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 189 Guo Shou Jing Rd, Shanghai 200062, Peoples R China
推荐引用方式 GB/T 7714	Shao, Pingxuan,Zhou, Yan,Yang, Dehua,et al. Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs[J]. MOLECULES,2019,24(23):13.
APA	Shao, Pingxuan,Zhou, Yan,Yang, Dehua,Wang, Ming-Wei,Lu, Wei,&Jin, Jiyu.(2019).Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs.MOLECULES,24(23),13.
MLA	Shao, Pingxuan,et al."Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs".MOLECULES 24.23(2019):13.