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Synthesis, Structure−Activity Relationships, and Characterization of Novel Nonsteroidal and Selective Androgen Receptor Modulators

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posted on 26.11.2009 by Nathalie Schlienger, Birgitte W. Lund, Jan Pawlas, Fabrizio Badalassi, Fabio Bertozzi, Rasmus Lewinsky, Alma Fejzic, Mikkel B. Thygesen, Ali Tabatabaei, Stefania Risso Bradley, Luis R. Gardell, Fabrice Piu, Roger Olsson
Herein we describe the discovery of ACP-105 (1), a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone. Compound 1 was developed from a series of compounds found in a HTS screen using the receptor selection and amplification technology (R-SAT). In vivo, 1 improved anabolic parameters in a 2-week chronic study in castrated male rats. In addition to compound 1, a number of potent antiandrogens were discovered from the same series of compounds whereof one compound, 13, had antagonist activity at the AR T877A mutant involved in prostate cancer.

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