Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
Article Details
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Zhao S, Shen Y, van Oeveren A, Marschke KB, Zhi L
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. Epub 2008 Apr 8.
- PubMed ID
- 18442912 [ View in PubMed]
- 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Bicalutamide Androgen receptor IC 50 (nM) 162 N/A N/A Details Bicalutamide Androgen receptor Ki (nM) 151 N/A N/A Details Bicalutamide Androgen receptor IC 50 (nM) 232 N/A N/A Details Bicalutamide Androgen receptor EC 50 (nM) >10000 N/A N/A Details Stanolone Androgen receptor IC 50 (nM) >10000 N/A N/A Details Stanolone Androgen receptor EC 50 (nM) 5.1 N/A N/A Details Stanolone Androgen receptor Ki (nM) 0.2 N/A N/A Details Stanolone Androgen receptor IC 50 (nM) 0.05 N/A N/A Details