Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).

@article{Mitchell2009DesignSA,
  title={Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).},
  author={Helen J Mitchell and William P Dankulich and George D. Hartman and Thomayant Prueksaritanont and Azriel Schmidt and Robert L. Vogel and Chang Bai and Sheila McElwee-Witmer and Hai Zhuan Zhang and Fang Chen and Chih-Tai Leu and Donald B. Kimmel and William J. Ray and Pascale V. Nantermet and Michael A Gentile and Mark E. Duggan and Robert S Meissner},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 15},
  pages={4578-81}
}
A novel series of 16-substituted-4-azasteroids has been identified as potential tissue-selective androgen receptor modulators. These ligands display potent hAR binding and agonist activity, low virilizing potential, and good pharmacokinetic profiles in dogs. On the basis of its in vitro profile, 21 was evaluated in the OVX and ORX rat models and exhibited… CONTINUE READING