Results 251 to 260 of about 18,995 (290)
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The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists
Bioorganic and Medicinal Chemistry Letters, 2004A novel series of [2.2.1]-azahydantoins has been designed and synthesized in an enantiospecific manner. The ability of these compounds to act as antagonists to the androgen receptor was investigated and several were found to have potent activity in vitro.
Aaron Balog +2 more
exaly +3 more sources
Androgen receptor antagonists: a patent review (2008 – 2011)
Expert Opinion on Therapeutic Patents, 2012Androgen 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 +2 more
exaly +3 more sources
Advances in the computational development of androgen receptor antagonists
Drug Discovery Today, 2020The 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 +7 more
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Recent Androgen Receptor Antagonists in Prostate Cancer
Mini-Reviews in Medicinal Chemistry, 2014Androgen receptor has been shown to promote prostate cell growth and carcinogenesis of prostate cancer by up-regulating its target genes. Testosterone and dihydrotestosterone are two major hormones which bind to and activate androgen receptor. Targeting both the androgen receptor and the enzymes catalyzing the biosynthesis of testosterone and ...
Xufang, Lu +5 more
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Steroid derivatives as pure antagonists of the androgen receptor
The Journal of Steroid Biochemistry and Molecular Biology, 2012While 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 +2 more
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Peptide Antagonist of the Androgen Receptor
Current Pharmaceutical Design, 2010Androgen receptor (AR) is a steroid hormone receptor that is activated by endogenous androgens, mainly testosterone and 5alpha-dihydrotestosterone (5alpha-DHT). AR is also an important drug target, and AR antagonists (antiandrogens) have been widely used for prostate cancer therapy.
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2010
Androgen receptor (AR) antagonists used clinically include steroidal (cyproterone acetate) and nonsteroidal antagonists (bicalutamide, flutamide, and nilutamide), with the latter nonsteroidal compounds being the only ones in general use in the United States. AR antagonists are used as single agents or in conjunction with surgical or medical castration (
Howard C. Shen +2 more
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Androgen receptor (AR) antagonists used clinically include steroidal (cyproterone acetate) and nonsteroidal antagonists (bicalutamide, flutamide, and nilutamide), with the latter nonsteroidal compounds being the only ones in general use in the United States. AR antagonists are used as single agents or in conjunction with surgical or medical castration (
Howard C. Shen +2 more
openaire +1 more source
Androgens and acne: perspectives on clascoterone, the first topical androgen receptor antagonist
Expert Opinion on Pharmacotherapy, 2021Introduction: 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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A Chemoenzymatic Synthesis of an Androgen Receptor Antagonist
Organic Process Research & Development, 2007A new scalable enzymatic resolution approach to both enantiomers of trans-2-hydroxycyclohexanecarbonitrile (9 and 11) was developed. Treatment of the racemic mixture (4) with succinic anhydride in the presence of Novozym 435 led to selective acylation of one enantiomer to the corresponding hemisuccinate, which was separated from the unreacted ...
Rajappa Vaidyanathan +2 more
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TAS3681: New class of androgen receptor antagonist with androgen receptor downregulating activity.
Journal of Clinical Oncology, 2015266 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 +10 more
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