2. Academic Validation
  3. Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones

Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones

  • Bioorg Med Chem Lett. 2008 Jun 1;18(11):3431-5. doi: 10.1016/j.bmcl.2008.03.085.
Shuo Zhao 1,  Yixing Shen,  Arjan van Oeveren,  Keith B Marschke,  Lin Zhi
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, CA 92121, USA. szhao2005@gmail.com
PMID: 18442912 DOI: 10.1016/j.bmcl.2008.03.085
Abstract

A novel oxachrysenone series (2) of nonsteroidal selective Androgen Receptor modulators (SARM) was developed based on the 6-aryl-2-quinolinones (1). Synthesis and preliminary SAR results based on in vitro assays are discussed. In the cotransfection assay, lead compound 5d showed AR agonist activity more potent than dihydrotestosterone (DHT), whereas compound 17b was a potent antagonist similar to bicalutamide.

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