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- Title
Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs.
- Authors
Shao, Pingxuan; Zhou, Yan; Yang, Dehua; Wang, Ming-Wei; Lu, Wei; Jin, Jiyu
- Abstract
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.
- Subjects
ANDROGEN receptors; PHARMACEUTICAL chemistry; CLINICAL trials
- Publication
Molecules, 2019, Vol 24, Issue 23, p4227
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules24234227