Aromatic beta-amino-ketone derivatives as novel selective non-steroidal progesterone receptor antagonists.
A novel class of non-steroidal progesterone receptor antagonists with aromatic beta-amino-ketone scaffold have been synthesized and characterized with high binding affinity and great selectivity for the cognate receptors. Among them, compound 22 was shown to be the most potent progesterone receptor antagonist in cotransfection assay and a murine model of ligand-induced decidualization.
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, PR China.
Yongli
Y
Du
Qunyi
Q
Li
Bing
B
Xiong
Xin
X
Hui
Xin
X
Wang
Yang
Y
Feng
Tao
T
Meng
Dingyu
D
Hu
Datong
D
Zhang
Mingwei
M
Wang
Jingkang
J
Shen
D000814:Aniline Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000818:Animals; D001665:Binding Sites; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D003198:Computer Simulation; D018360:Crystallography, X-Ray; D006801:Humans; D007659:Ketones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008024:Ligands; D051379:Mice; D008968:Molecular Conformation; D011485:Protein Binding; D011980:Receptors, Progesterone / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
C552760:3-(4-nitrophenylamino)-3-(3-fluorophenyl)-1-p-tolylpropan-1-one; D000814:Aniline Compounds; D047188:Chalcones; D007659:Ketones; D008024:Ligands; D011980:Receptors, Progesterone