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

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. 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.