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

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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
DrugTargetPropertyMeasurementpHTemperature (°C)
BicalutamideAndrogen receptorIC 50 (nM)162N/AN/ADetails
BicalutamideAndrogen receptorKi (nM)151N/AN/ADetails
BicalutamideAndrogen receptorIC 50 (nM)232N/AN/ADetails
BicalutamideAndrogen receptorEC 50 (nM)>10000N/AN/ADetails
StanoloneAndrogen receptorIC 50 (nM)>10000N/AN/ADetails
StanoloneAndrogen receptorEC 50 (nM)5.1N/AN/ADetails
StanoloneAndrogen receptorKi (nM)0.2N/AN/ADetails
StanoloneAndrogen receptorIC 50 (nM)0.05N/AN/ADetails