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    Bioorg Med Chem Lett. 2008 Jun 1;18(11):3431-5. Epub 2008 Apr 8.

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

    Zhao S, Shen Y, van Oeveren A, Marschke KB, Zhi L.

    Discovery Research, Ligand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, CA 92121, USA. szhao2005@gmail.com

    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.

    PMID: 18442912 [PubMed - indexed for MEDLINE]

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