Literature DB >> 10230629

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

L Zhi1, C M Tegley, K B Marschke, T K Jones.   

Abstract

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.

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Year:  1999        PMID： 10230629     DOI： 10.1016/s0960-894x(99)00119-5

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

Review 1.  Chemistry and structural biology of androgen receptor.

Authors:  Wenqing Gao; Casey E Bohl; James T Dalton
Journal:  Chem Rev       Date:  2005-09       Impact factor: 60.622

Review 2.  Discovery and therapeutic promise of selective androgen receptor modulators.

Authors:  Jiyun Chen; Juhyun Kim; James T Dalton
Journal:  Mol Interv       Date:  2005-06

3.  Enantioselective γ-C(sp3)-H Activation of Alkyl Amines via Pd(II)/Pd(0) Catalysis.

Authors:  Qian Shao; Qing-Feng Wu; Jian He; Jin-Quan Yu
Journal:  J Am Chem Soc       Date:  2018-04-11       Impact factor: 15.419

Review 4.  Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands.

Authors:  Wenqing Gao; Juhyun Kim; James T Dalton
Journal:  Pharm Res       Date:  2006-08       Impact factor: 4.200

5.  Design, synthesis, and biological characterization of metabolically stable selective androgen receptor modulators.

Authors:  Craig A Marhefka; Wenqing Gao; Kiwon Chung; Juhyun Kim; Yali He; Donghua Yin; Casey Bohl; James T Dalton; Duane D Miller
Journal:  J Med Chem       Date:  2004-02-12       Impact factor: 7.446

6.  A ligand-based approach to identify quantitative structure-activity relationships for the androgen receptor.

Authors:  Casey E Bohl; Cheng Chang; Michael L Mohler; Jiyun Chen; Duane D Miller; Peter W Swaan; James T Dalton
Journal:  J Med Chem       Date:  2004-07-15       Impact factor: 7.446

7.  Global analysis of small molecule binding to related protein targets.

Authors:  Felix A Kruger; John P Overington
Journal:  PLoS Comput Biol       Date:  2012-01-12       Impact factor: 4.475

8.  Discovery and Identification of Pyrazolopyramidine Analogs as Novel Potent Androgen Receptor Antagonists.

Authors:  Lingyan Wang; Tianqing Song; Xin Wang; Jiazhong Li
Journal:  Front Pharmacol       Date:  2018-08-28       Impact factor: 5.810

9.  Synthesis of N-aryl β-amino acid derivatives via Cu(ii)-catalyzed asymmetric 1,4-reduction in air.

Authors:  Min Li; Hong-Feng Xia; Li-Yao Yang; Tao Hong; Lin-Jie Xie; Shijun Li; Jing Wu
Journal:  RSC Adv       Date:  2019-03-20       Impact factor: 4.036
  9 in total

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