Article
Development of Androgen-Antagonistic Coumarinamides with a Unique Aromatic Folded Pharmacophore.
International journal of molecular sciences - 4 Aug 2020
Koga Hitomi, Negishi Mai, Kinoshita Marie, Fujii Shinya, Mori Shuichi, Ishigami-Yuasa Mari, Kawachi Emiko, Kagechika Hiroyuki, Tanatani Aya
Abstract excerpt
First-generation nonsteroidal androgen receptor (AR) antagonists, such as flutamide (2a) and bicalutamide (3), are effective for most prostate cancer patients, but resistance often appears after several years due to the mutation of AR. Second-generation AR antagonists are effective against some of these castration-resistant prostate cancers, but their structural variety is still limited. In this study, we...
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