Results 211 to 220 of about 17,593 (256)

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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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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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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Androgens and acne: perspectives on clascoterone, the first topical androgen receptor antagonist

Expert Opinion on Pharmacotherapy, 2021
Introduction: Increased circulating androgens are key to the multifactorial pathogenesis of acne. Clascoterone is the first topical androgen antagonist developed to treat acne in both male and female patients and the first such agent to receive U.S. Food and Drug Administration (FDA) approval for treatment of acne.
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TAS3681: New class of androgen receptor antagonist with androgen receptor downregulating activity.

Journal of Clinical Oncology, 2015
266 Background: The persistent activation of the androgen receptor (AR) signaling axis plays a major role in castration-resistant prostate cancer (CRPC). This knowledge has driven the clinical development of new inhibitors of androgen production (e.g., abiraterone) and AR signaling (e.g., enzalutamide).
Kazuhisa Minamiguchi, Masanao Seki, Hiroki Aoyagi, Daisuke Kajiwara, Tomoko Mori, Norio Masuko, Ryouto Fujita, Shigeo Okajima, Yukio Hayashi, Eiji Sasaki, Teruhiro Utsugi   +10 more
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Cimetidine, a Histamine H₂Receptor Antagonist, Occupies Androgen Receptors*

The Journal of Clinical Endocrinology & Metabolism, 1979
The histamine H2 receptor antagonist cimetidine is in increasing usage in the medical management of peptic ulcer. In clinical trials, its most frequent side effect is gynecomastia. Such estrogenic/antiandrogenic manifestations are well known side effects of treatment with digitoxin or spirolactones.
J W, Funder, J E, Mercer
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Resistance to second-generation androgen receptor antagonists in prostate cancer

Nature Reviews Urology, 2021
The introduction of second-generation androgen receptor antagonists (SG-ARAs) has greatly impacted the treatment of metastatic prostate cancer, providing tolerable and efficacious alternatives to chemotherapy. SG-ARAs provide similar therapeutic benefit to abiraterone, a potent CYP17 inhibitor, and do not require the co-administration of prednisone ...
Keith T. Schmidt, Alwin D. R. Huitema, Cindy H. Chau, William D. Figg   +3 more
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Rational drug design for androgen receptor and glucocorticoids receptor dual antagonist

European Journal of Medicinal Chemistry, 2019
Prostate cancer (PCa) is the most frequently diagnosed male malignant tumor and remains the second leading cause of male cancer mortality in the western countries. The second-generation antiandrogen enzalutamide (ENZa) can prolong survival time for patients with mCRPC.
Meng Wu, Yongli Xie, Xiangling Cui, Chenchao Huang, Rongyu Zhang, Yang He, Xiaoyu Li, Mingliang Liu, Shan Cen, Jinming Zhou   +9 more
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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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