Article
Synthesis and in vitro characterization of ionone-based chalcones as novel antiandrogens effective against multiple clinically relevant androgen receptor mutants.
Investigational new drugs - 1 Jun 2010
Zhou Jinming, Geng Guoyan, Wu Jian Hui
Abstract excerpt
A crucial event in prostate cancer progression is the transition from a hormone-sensitive to a lethal castration-refractory disease state. The antagonist-to-agonist conversion due to mutation in AR is a critical problem with the current clinically used antiandrogens. We aim to identify novel antiandrogens that remain as a pure antagonist even in the mutated ARs. By synthesizing a series of ionone-based chalcones,...
Topics
- Androgen Antagonists
- Androgen Receptor Antagonists
- Antineoplastic Agents, Hormonal
- Cell Line, Tumor
- Cell Proliferation
- Chalcones
- Drug Design
- Drug Resistance, Neoplasm
- Drug Screening Assays, Antitumor
- Humans
- Male
- Molecular Structure
- Mutation
- Norisoprenoids