ArticleJournal of medicinal chemistry2017
1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment.
Article in Journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
9 citing papers in PubMed, 55 citations in OpenAlex.
- Synthesis of Novel Aminothiazole Derivatives as Promising Antiviral, Antioxidant and Antibacterial Candidates.International journal of molecular sciences · 2022Article
- Amidine- and Amidoxime-Substituted Heterocycles: Synthesis, Antiproliferative Evaluations and DNA Binding.Molecules (Basel, Switzerland) · 2021Article
- New Selective Inhibitors of ERG Positive Prostate Cancer: ERGi-USU-6 Salt Derivatives.ACS medicinal chemistry letters · 2021Article
- miRNAs as Therapeutic Tools and Biomarkers for Prostate Cancer.Pharmaceutics · 2021Review
- Synthesis and preclinical validation of novel P2Y1 receptor ligands as a potent anti-prostate cancer agent.Scientific reports · 2019Article
- NewRSC advances · 2019Article
- Design, Synthesis, and Biological Evaluation of (E)-N'-((1-Chloro-3,4-Dihydronaphthalen-2-yl)Methylene)Benzohydrazide Derivatives as Anti-prostate Cancer Agents.Frontiers in chemistry · 2019Article
- Androgen Receptor-Directed Molecular Conjugates for Targeting Prostate Cancer.Frontiers in chemistry · 2019Review
- Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents.MedChemComm · 2017Article
Corrections and comments
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Authors and funding
15 authors at 6 institutions in 2 countries.
Funding
Abstract
Prostate cancer (PC) is the fifth leading cause of cancer death in men, and the androgen receptor (AR) represents the primary target for PC treatment, even though the disease frequently progresses toward androgen-independent forms. Most of the commercially available nonsteroidal antiandrogens show a common scaffold consisting of two aromatic rings connected by a linear or a cyclic spacer. By taking advantage of a facile, one-pot click chemistry reaction, we report herein the preparation of a small library of novel 1,4-substituted triazoles with AR antagonistic activity. Biological and theoretical evaluation demonstrated that the introduction of the triazole core in the scaffold of nonsteroidal antiandrogens allowed the development of small molecules with improved overall AR-antagonist activity. In fact, compound 14d displayed promising in vitro antitumor activity toward three different prostate cancer cell lines and was able to induce 60% tumor growth inhibition of the CW22Rv1 in vivo xenograft model. These results represent a step toward the development of novel and improved AR antagonists.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.