Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure.
Synthesis and structure-activity relationship of RXR antagonists employing a diazepinylbenzoic acid scaffold are described. Of those antagonists, sulfonamide derivatives (6v and 6w) reveal a high antagonistic activity and good pharmacokinetic properties.
Sakaki
Junichi
J
Novartis Institute for Biomedical Research, Tsukuba Research Institute, Ohkubo 8, Tsukuba-Shi, Ibaraki, Japan.
Konishi
Kazuhide
K
Kishida
Masashi
M
Gunji
Hiroki
H
Kanazawa
Takanori
T
Uchiyama
Hidefumi
H
Fukaya
Hiroaki
H
Mitani
Hironobu
H
Kimura
Masaaki
M
D000284:Administration, Oral; D001565:Benzoates / Q000138:chemical synthesis* / Q000737:chemistry*; D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015394:Molecular Structure; D018168:Receptors, Retinoic Acid / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D000072482:Retinoic Acid Receptor alpha; D013329:Structure-Activity Relationship; D013997:Time Factors; D015534:Trans-Activators; D014157:Transcription Factors / Q000737:chemistry; D015533:Transcriptional Activation
D001565:Benzoates; D001713:Biphenyl Compounds; C000607071:RARA protein, human; D018168:Receptors, Retinoic Acid; D000072482:Retinoic Acid Receptor alpha; D015534:Trans-Activators; D014157:Transcription Factors; C438269:diazepinylbenzoic acid