Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists
Copyright policy )Discovery of Aryloxy Tetramethylcyclobutanes as Novel Androgen Receptor Antagonists
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 growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model.
- Vancouver Prostate Centre Canada
- Pfizer (United States) United States
- Pfizer (United Kingdom) United Kingdom
- University of British Columbia Canada
Male, Models, Molecular, Administration, Oral, Mice, Nude, Prostatic Neoplasms, Androgen Antagonists, Antineoplastic Agents, Bridged Bicyclo Compounds, Heterocyclic, Ligands, Xenograft Model Antitumor Assays, Cell Line, High-Throughput Screening Assays, Mice, Structure-Activity Relationship, Drug Resistance, Neoplasm, Androgens, Animals, Humans, Pyrazoles, Cyclobutanes
Male, Models, Molecular, Administration, Oral, Mice, Nude, Prostatic Neoplasms, Androgen Antagonists, Antineoplastic Agents, Bridged Bicyclo Compounds, Heterocyclic, Ligands, Xenograft Model Antitumor Assays, Cell Line, High-Throughput Screening Assays, Mice, Structure-Activity Relationship, Drug Resistance, Neoplasm, Androgens, Animals, Humans, Pyrazoles, Cyclobutanes
selected citations These citations are derived from selected sources.This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).67 popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.Top 10% influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).Top 10% impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.Top 10%
Citations provided by BIP!Popularity provided by BIP!