Issue 9, 2011
From the journal:

MedChemComm

p-Carborane-based androgen antagonists active in LNCaPcells with a mutated androgen receptor†

Shinya Fujii,a   Ayumi Yamada,a   Keiko Tomita,b   Mao Nagano,b   Tokuhito Goto,c   Kiminori Ohta,c   Takashi Harayama,b   Yasuyuki Endoc  and  Hiroyuki Kagechika*a  

* Corresponding authors

a Graduate School of Biomedical Science, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10, Kanda-Surugadai, Chiyoda-ku, Tokyo, Japan
E-mail: kage.omc@tmd.ac.jp
Fax: +81-3-5280-8127
Tel: +81-3-5280-8032

b Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, 1314-1,Shido, Sanuki, Kagawa, Japan

c Faculty of Pharmaceutical Sciences, Tohoku Pharmaceutical University, 4-4-1, Komatsushima, Aoba-ku, Sendai, Japan

Abstract

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.

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

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Article information

DOI
https://doi.org/10.1039/C1MD00001B
Article type
Concise Article
Submitted
05 Jan 2011
Accepted
17 Jun 2011
First published
21 Jul 2011

Med. Chem. Commun., 2011,2, 877-880

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

S. Fujii, A. Yamada, K. Tomita, M. Nagano, T. Goto, K. Ohta, T. Harayama, Y. Endo and H. Kagechika, Med. Chem. Commun., 2011, 2, 877 DOI: 10.1039/C1MD00001B

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