2. Academic Validation
  3. Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones

Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones

  • Bioorg Med Chem Lett. 2007 Mar 15;17(6):1523-6. doi: 10.1016/j.bmcl.2007.01.007.
Arjan van Oeveren 1,  Barbara A Pio,  Christopher M Tegley,  Robert I Higuchi,  Min Wu,  Todd K Jones,  Keith B Marschke,  Andrés Negro-Vilar,  Lin Zhi
Affiliations

Affiliation

  • 1 Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA.
PMID: 17257838 DOI: 10.1016/j.bmcl.2007.01.007
Abstract

A series of alkylamino-2-quinolinone compounds (3) was discovered as Androgen Receptor modulators based on an early linear tricyclic quinoline pharmacophore (1). The series demonstrated selective high binding affinity to Androgen Receptor and potent receptor modulating activities in the cotransfection assays.

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