Results 221 to 230 of about 19,533 (266)

Classification and Virtual Screening of Androgen Receptor Antagonists

Journal of Chemical Information and Modeling, 2010
Computational tools, such as quantitative structure-activity relationship (QSAR), are highly useful as screening support for prioritization of substances of very high concern (SVHC). From the practical point of view, QSAR models should be effective to pick out more active rather than inactive compounds, expressed as sensitivity in classification works.
Jiazhong, Li, Paola, Gramatica
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Androgen Antagonists

2007
Androgens are essential for the development and maintenance of male sexual characteristics. They exert their effects through the androgen receptor, which is a member of the …
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Androgen antagonists: Potential role in prostate cancer prevention

Urology, 2001
This article summarizes discussions of the importance of androgens and androgen antagonists in the genesis of prostate cancer. These discussions occurred at a recent symposium on prostate cancer chemoprevention sponsored by the National Cancer Institute.
D L, Trump, J A, Waldstreicher, G, Kolvenbag, P S, Wissel, B L, Neubauer   +4 more
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Advances in the computational development of androgen receptor antagonists

Drug Discovery Today, 2020
The androgen receptor is a ligand-dependent transcriptional factor and an essential therapeutic target for prostate cancer. Competitive binding of antagonists to the androgen receptor can alleviate aberrant activation of the androgen receptor in prostate cancer.
Xueping Hu, Xin Chai, Xuwen Wang, Mojie Duan, Jinping Pang, Weitao Fu, Dan Li, Tingjun Hou   +7 more
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Androgen receptor antagonists: a patent review (2008 – 2011)

Expert Opinion on Therapeutic Patents, 2012
Androgen receptor (AR) antagonists are predominantly used as chemical castration to treat prostate cancer (i.e., in conjunction with androgen deprivation therapy (ADT)). Unfortunately, castration-resistant prostate cancer (CRPC) typically develops that is refractory to targeted therapy.
Michael L, Mohler, Christopher C, Coss, Charles B, Duke, Shivaputra A, Patil, Duane D, Miller, James T, Dalton   +5 more
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Preliminary investigations into triazole derived androgen receptor antagonists

Bioorganic & Medicinal Chemistry, 2014
A range of 1,4-substituted-1,2,3-N-phenyltriazoles were synthesized and evaluated as non-steroidal androgen receptor (AR) antagonists. The motivation for this study was to replace the N-phenyl amide portion of small molecule antiandrogens with a 1,2,3-triazole and determine effects, if any, on biological activity.
Altimari, Jarrad, Niranjan, Birunthi, Risbridger, Gail, Schweiker, Stephanie, Lohning, Anna, Henderson, Luke   +5 more
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[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2016
This letter describes the discovery, synthesis, SAR, and biological activity of [2.2.1]-bicyclic sultams as potent antagonists of the androgen receptor. Optimization of the series led to the identification of compound 25, which displayed robust pharmacodynamic effects in rats after oral dosing.
Weifang Shan, Aaron Balog, Andrew Nation, Xiao Zhu, Jing Chen, Mary Ellen Cvijic, Jieping Geng, Cheryl A. Rizzo, Thomas Spires, Ricardo M. Attar, Mary Obermeier, Sarah Traeger, Jun Dai, Yingru Zhang, Michael Galella, George Trainor, Gregory D. Vite, Ashvinikumar V. Gavai   +17 more
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Antagonistic effect of androgen on prostatic cell death

The Prostate, 1984
AbstractAndrogen, besides having the well‐established agonistic ability to stimulate prostate cell proliferation, also has an antagonistic ability to inhibit prostatic cell death. This statement is based upon the observations that 1) only 2.1% of the total prostatic cells die per day when serum testosterone level is sufficient for chronic maintenance ...
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Steroid derivatives as pure antagonists of the androgen receptor

The Journal of Steroid Biochemistry and Molecular Biology, 2012
While the androgens of testicular origin (representing about 50% of total androgens in men over 50 years) can be completely eliminated by surgical or medical castration with GnRH (gonadotropin-releasing hormone) agonists or antagonists, the antiandrogens currently available as blockers of androgen binding to the androgen receptor (AR), namely ...
Sylvain, Gauthier, Céline, Martel, Fernand, Labrie   +2 more
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Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists

Journal of Medicinal Chemistry, 2011
An aryloxy tetramethylcyclobutane was identified as a novel template for androgen receptor (AR) antagonists via cell-based high-throughput screening. Follow-up to the initial "hit" established 5 as a viable lead. Further optimization to achieve full AR antagonism led to the discovery of 26 and 30, both of which demonstrated excellent in vivo tumor ...
Chuangxing, Guo, Angelica, Linton, Susan, Kephart, Martha, Ornelas, Mason, Pairish, Javier, Gonzalez, Samantha, Greasley, Asako, Nagata, Benjamin J, Burke, Martin, Edwards, Natilie, Hosea, Ping, Kang, Wenyue, Hu, Jon, Engebretsen, David, Briere, Manli, Shi, Hovik, Gukasyan, Paul, Richardson, Kevin, Dack, Toby, Underwood, Patrick, Johnson, Andrew, Morell, Robert, Felstead, Hidetoshi, Kuruma, Hiroaki, Matsimoto, Amina, Zoubeidi, Martin, Gleave, Gerrit, Los, Andrea N, Fanjul   +28 more
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