p-Carborane-based androgen antagonists active in LNCaP cells with a mutated androgen receptor

Development of antagonists for a mutated androgen receptor (AR) is important for treatment of anti-androgen-refractory prostate cancers. We describe here application of the p-carborane cage as a hydrophobic core structure for novel anti-androgens active toward LNCaP human prostate cancer cells with mutated AR. These compounds are expected to be versatile lead compounds not only for development of AR pan-antagonists, but also for discovery of mutant-selective anti-androgens.