Results 261 to 270 of about 18,995 (290)

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
openaire   +2 more sources

Androgen Receptor Antagonists (Antiandrogens) Structure-Activity Relationships

Current Medicinal Chemistry, 2000
Prostate cancer, acne, seborrhea, hirsutism, and androgenic alopecia are well recognized to depend upon an excess or increased sensitivity to androgens or to be at least sensitive to androgens. It thus seems logical to use antiandrogens as therapeutic agents to prevent androgens from binding to the androgen receptor.
S M, Singh, S, Gauthier, F, Labrie
openaire   +2 more sources

Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists

Bioorganic & Medicinal Chemistry Letters, 2012
Oxobenzimidazoles (e.g., 1), a novel series of androgen receptor (AR) antagonists, were discovered through de novo design guided by structure-based drug design. The compounds in this series were reasonably permeable and metabolically stable, but suffered from poor solubility.
Chuangxing, Guo, Mason, Pairish, Angelica, Linton, Susan, Kephart, Martha, Ornelas, Asako, Nagata, Benjamin, Burke, Liming, Dong, Jon, Engebretsen, Andrea N, Fanjul   +9 more
openaire   +2 more sources

Stabilization of androgen receptor protein is induced by agonist, not by antagonists

Biochemical and Biophysical Research Communications, 2002
The action of nuclear receptor ligands in target tissues is specified mainly by the expression levels of their cognate nuclear receptors. The expression levels of these receptors are controlled through transcriptional and post-transcriptional events.
Takashi, Furutani, Tomoyuki, Watanabe, Kyouko, Tanimoto, Takamichi, Hashimoto, Hiroshi, Koutoku, Masafumi, Kudoh, Yasuaki, Shimizu, Shigeaki, Kato, Hisataka, Shikama   +8 more
openaire   +2 more sources

[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
openaire   +2 more sources

Functional Activities of the A and B Forms of the Human Androgen Receptor in Response to Androgen Receptor Agonists and Antagonists

Molecular Endocrinology, 1998
AbstractThe androgen receptor (AR) is present in many cells in two forms. The B form migrates with an apparent mass of 110 kDa and constitutes more than 80% of the immunoreactive receptor in most cell types. The A form of the AR migrates with an apparent mass of 87 kDa, appears to derive from internal translation initiation at methionine-188 in the AR ...
T, Gao, M J, McPhaul
openaire   +2 more sources

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
openaire   +2 more sources

Synthesis of the Androgen-Receptor Antagonists (±)-Ws9761 A and B

Australian Journal of Chemistry, 1996
The non-steroidal androgen-receptor antagonists WS9761 A (1,6,10-trihydroxy-2,8,10-trimethylanthrone) and WS9761 B (1,6,10-trihydroxy-2-hydroxymethyl-8,10-dimethylanthrone) were synthesized for the first time in racemic form by using Diels-Alder methodology followed by regioselective Grignard addition.
DW Cameron, CE Skene
openaire   +1 more source

Design, synthesis and biological evaluation of novel thiohydantoin derivatives as potent androgen receptor antagonists for the treatment of prostate cancer

Bioorganic and Medicinal Chemistry, 2021
Yushe Yang
exaly  

Binary and multi-class classification for androgen receptor agonists, antagonists and binders

Chemosphere, 2021
Geven Piir, Sulev Sild, Uko Maran
exaly