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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor
Helen J Mitchell1, William P Dankulich, George D Hartman
1Department of Medicinal Chemistry, Merck Research Laboratories, P.O. Box 4, 770 Sumneytown Pike, West Point, Pennsylvania 19486, USA. Helen_mitchell2@merck.com
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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