p-Carborane Based AndrogenActive in LNCaP Cells with a Mutated Androgen Receptor

p-Carborane Based AndrogenActive in LNCaP Cells with a Mutated Androgen Receptor
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基于对碳硼烷的雄激素在雄激素受体突变的 LNCaP 细胞中具有活性

DOI：
10.1039/c1md00001b
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发表时间：
2011
期刊：
Med. Chem. Commun
影响因子：
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通讯作者：
Hiroyuki Kagechika
Hiroyuki Kagechika
中科院分区：
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文献类型：
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作者：
Shinya Fujii;Ayumi Yamada;Keiko Tomita;Mao Nagano;Tokuhito Goto;Kiminori Ohta;Takashi Harayama;Yasuyuki Endo;Hiroyuki Kagechika

文献摘要

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雄激素受体(AR)突变拮抗剂的开发对抗雄激素耐药前列腺癌的治疗具有重要意义。在这里，我们描述了p-Carborane笼子作为疏水核心结构的应用，用于对具有突变AR的LNCaP人前列腺癌细胞具有活性的新型抗雄激素。这些化合物有望成为多用途的先导化合物，不仅可用于AR泛拮抗剂的开发，还可用于发现突变体选择性的抗雄激素。
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.