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Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs.

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.

SUBMITTER: Shao P 

PROVIDER: S-EPMC6930600 | biostudies-literature | 2019 Nov

REPOSITORIES: biostudies-literature

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Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs.

Shao Pingxuan P   Zhou Yan Y   Yang Dehua D   Wang Ming-Wei MW   Lu Wei W   Jin Jiyu J  

Molecules (Basel, Switzerland) 20191120 23

The pentafluorosulfane (SF<sub>5</sub>) group, as a more electronegative bioisostere than the trifluoromethyl (CF<sub>3</sub>) group, has been gaining greater attention and increasingly reported usage in medicinal chemistry. Ostarine is the selective androgen receptor modulators (SARMs) containing a CF<sub>3</sub> group in clinical trial III. In this study, 21 ostarine derivatives for replacing the CF<sub>3</sub> group with SF<sub>5</sub> substituents were synthesized. Some SF<sub>5</sub>-deriva  ...[more]

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