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Discovery of an androgen receptor modulator pharmacophore based on 2-quinolinones |
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| Authors: | van Oeveren Arjan Pio Barbara A Tegley Christopher M Higuchi Robert I Wu Min Jones Todd K Marschke Keith B Negro-Vilar Andrés Zhi Lin |
| Institution: | Discovery Research, Ligand Pharmaceuticals, 10275 Science Center Drive, San Diego, CA 92121, USA. |
| 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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