Synthesis of Hydantoin Androgen Receptor Antagonists and Study on Their Antagonistic Activity [PDF]
Molecules, 2022 Hydroxymethylthiohydantoin, hydroxymethylthiohydantoin, and hydantoin, containing a pyridine group, were synthesized to study their androgen receptor antagonistic activities.
Longjun Ma +5 more
doaj +4 more sources
CREB5 Promotes Resistance to Androgen-Receptor Antagonists and Androgen Deprivation in Prostate Cancer [PDF]
Cell Reports, 2019 Summary: Androgen-receptor (AR) inhibitors, including enzalutamide, are used for treatment of all metastatic castration-resistant prostate cancers (mCRPCs). However, some patients develop resistance or never respond. We find that the transcription factor
Justin H. Hwang +31 more
doaj +4 more sources
Similarities and Distinctions in Actions of Surface-Directed and Classic Androgen Receptor Antagonists. [PDF]
PLoS ONE, 2015 The androgen receptor (AR) surface-directed antagonist MJC13 inhibits AR function and proliferation of prostate cancer (PC) cells. These effects are related to arrest of an AR/chaperone complex in the cytoplasm.
Ji Ho Suh +5 more
doaj +3 more sources
Design, synthesis, and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonists [PDF]
Journal of Enzyme Inhibition and Medicinal Chemistry, 2019 Prostate cancer (PCa) is the second leading cause of death in men. Apart from androgen receptor, 5α-reductase has also been recognized as a potential target.
Kejing Lao +3 more
doaj +3 more sources
The epigenetic function of androgen receptor in prostate cancer progression [PDF]
Frontiers in Cell and Developmental Biology, 2023 Androgen and androgen deprivation (castration) therapies, including androgen receptor antagonists, are clinically used to treat patients with prostate cancer.
Takahiro Sawada +9 more
doaj +2 more sources
In silico and in vitro assessment of androgen receptor antagonists
Computational Biology and Chemistry, 2021 There is a growing concern for male reproductive health as studies suggest that there is a sharp increase in prostate cancer and other fertility related problems.
Bereketoglu, Ceyhun, +3 more
core +4 more sources
International Journal of Molecular Sciences, 2012 Androgen receptor antagonists have been proved to be effective anti-prostate cancer agents. 3D-QSAR and Molecular docking methods were performed on curcumin derivatives as androgen receptor antagonists.
Guanhong Xu, Yanyan Chu
exaly +2 more sources
Identification of putative steroid receptor antagonists in bottled water: combining bioassays and high-resolution mass spectrometry. [PDF]
PLoS ONE, 2013 Endocrine disrupting chemicals (EDCs) are man-made compounds interfering with hormone signaling and thereby adversely affecting human health. Recent reports provide evidence for the presence of EDCs in commercially available bottled water, including ...
Martin Wagner +3 more
doaj +2 more sources
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 ...
Schweiker, Stephanie S. +5 more
core +3 more sources
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).
Li Jazhong, GRAMATICA, PAOLA
core +3 more sources