2. Academic Validation
  3. Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators

Synthesis, structure-activity relationships, and characterization of novel nonsteroidal and selective androgen receptor modulators

  • J Med Chem. 2009 Nov 26;52(22):7186-91. doi: 10.1021/jm901149c.
Nathalie Schlienger 1,  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
Affiliations

Affiliation

  • 1 ACADIA Pharmaceuticals AB, Medeon Science Park, S-205 12 Malmo, Sweden.
PMID: 19856921 DOI: 10.1021/jm901149c
Abstract

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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