Identification of equine in vitro metabolites of seven non‐steroidal selective androgen receptor modulators for doping control purposes

2021 ◽  
Author(s):  
Charlotte Cutler ◽  
Marjaana Viljanto ◽  
Polly Taylor ◽  
Pamela Hincks ◽  
Simon Biddle ◽  
...  
2021 ◽  
Author(s):  
Katarzyna Kowalczyk ◽  
Julio César Torres‐Elguera ◽  
Anna Jarek ◽  
Anna Konopka ◽  
Dorota Kwiatkowska ◽  
...  

2015 ◽  
Vol 7 (8) ◽  
pp. 673-683 ◽  
Author(s):  
Annelie Hansson ◽  
Heather Knych ◽  
Scott Stanley ◽  
Mario Thevis ◽  
Ulf Bondesson ◽  
...  

2012 ◽  
Vol 32 (9) ◽  
pp. 562-568 ◽  
Author(s):  
Oliver Krug ◽  
Andreas Thomas ◽  
Simon Beuck ◽  
Ina Schenk ◽  
Marc Machnik ◽  
...  

Molecules ◽  
2019 ◽  
Vol 24 (23) ◽  
pp. 4227
Author(s):  
Shao ◽  
Zhou ◽  
Yang ◽  
Wang ◽  
Lu ◽  
...  

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.


2019 ◽  
Author(s):  
Matthias Grill ◽  
Melanie Patt ◽  
Alex Odermatt

Anabolic androgenic steroids (AAS) are frequently used either clinically, by athletes, or for body shaping due to their muscle building and performance enhancing properties. AAS misuse is associated with cardiovascular diseases, mood changes and endocrine issues. Despite the recognition of the severe adverse effects of AAS misuse, the underlying molecular mechanisms are insufficiently understood. Selective androgen receptor modulators (SARMs) are supposed to diminish the adverse androgenic AAS effects while maximizing anabolic effects. In order to obtain androgen receptor modulating compounds of high purity for mechanistic in vitro investigations, this study summarizes protocols of optimized chemical synthesis for five AAS and two SARMs.


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