Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
Article Details
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Salvati ME, Balog A, Wei DD, Pickering D, Attar RM, Geng J, Rizzo CA, Hunt JT, Gottardis MM, Weinmann R, Martinez R
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
Bioorg Med Chem Lett. 2005 Jan 17;15(2):389-93.
- PubMed ID
- 15603960 [ View in PubMed]
- Abstract
A novel series of isoindoledione based compounds were identified as potent antagonists of the androgen receptor (AR). SAR around this series revealed dramatic differences in binding and function in mutant variants (MT) of the AR as compared to the wild type (WT) receptor. Optimization of the aniline portion revealed substitution patterns, which yielded potent antagonist activity against the WT AR as well as the MT AR found in the LNCaP and PCa2b human prostate tumor cell lines.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Bicalutamide Androgen receptor IC 50 (nM) 400 N/A N/A Details Bicalutamide Androgen receptor Ki (nM) 35 N/A N/A Details Bicalutamide Androgen receptor IC 50 (nM) 725 N/A N/A Details Bicalutamide Androgen receptor IC 50 (nM) 173 N/A N/A Details Bicalutamide Androgen receptor Ki (nM) 64 N/A N/A Details