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

…, M Wu, TK Jones, KB Marschke, A Negro-Vilar…

Index: van Oeveren, Arjan; Pio, Barbara A.; Tegley, Christopher M.; Higuchi, Robert I.; Wu, Min; Jones, Todd K.; Marschke, Keith B.; Negro-Vilar, Andres; Zhi, Lin Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 6 p. 1523 - 1526

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Citation Number: 28

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.