Bioorganic & Medicinal Chemistry Letters 1999-04-05

Switching androgen receptor antagonists to agonists by modifying C-ring substituents on piperidino[3,2-g]quinolinone.

L Zhi, C M Tegley, K B Marschke, T K Jones

文献索引：Bioorg. Med. Chem. Lett. 9(7) , 1009-12, (1999)

全文：HTML全文

摘要

New nonsteroidal human androgen receptor (hAR) agonists were developed from an hAR antagonist pharmacophore, 2(1H)-piperidino[3,2-g]quinolinone. (+/-)-trans-7,8-Diethyl-4-trifluoromethyl-2(H)-piperidino-[3,2-g]quinoli none was synthesized and demonstrated potent hAR agonist activity (EC50=3 nM) in the cell-based cotransfection assay and high binding affinity (Ki=16 nM) in the competitive receptor binding assay.

相关化合物

  • 反式-2-戊烯酸

相关文献：

Chemically engineering ligand selectivity at the free fatty acid receptor 2 based on pharmacological variation between species orthologs.

2012-12-01

[FASEB J. 26 , 4951-65, (2012)]

Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A).

2011-05-01

[Bioorg. Med. Chem. Lett. 21 , 2736-9, (2011)]

Structure-activity relationship of cinnamaldehyde analogs as inhibitors of AI-2 based quorum sensing and their effect on virulence of Vibrio spp.

2011-01-01

[PLoS ONE 6(1) , e16084, (2011)]

Production of functionalized polyhydroxyalkanoates by genetically modified Methylobacterium extorquens strains.

2010-01-01

[Microb. Cell Fact. 9 , 70, (2010)]

更多文献...