Literature DB >> 19606870

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

Helen J Mitchell1, William P Dankulich, George D Hartman, Thomayant Prueksaritanont, Azriel Schmidt, Robert L Vogel, Chang Bai, Sheila McElwee-Witmer, Hai Z Zhang, Fang Chen, Chih-Tai Leu, Donald B Kimmel, William J Ray, Pascale Nantermet, Michael A Gentile, Mark E Duggan, Robert S Meissner.   

Abstract

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 an osteoanabolic, tissue-selective profile.

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Year:  2009        PMID: 19606870     DOI: 10.1021/jm900880r

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  1 in total

1.  Mechanistic elucidation of the tandem Diels-Alder/(3 + 2) cycloadditions in the design and syntheses of heterosteroids.

Authors:  Benedicta Donkor; Abdul Rashid Umar; Ernest Opoku
Journal:  J Mol Model       Date:  2022-02-27       Impact factor: 1.810

  1 in total

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