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Issue 6, 2012
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Development of androgen receptor ligands by application of ten-vertex para-carborane as a novel hydrophobic core structure

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Abstract

We report here the design, synthesis, androgenic activity and anti-androgenic activity of novel derivatives of hexadecahedral 1,10-dicarba-closo-decaborane, which is generally called ten-vertex para-carborane. The synthesized compounds exhibited very high binding affinity for the androgen receptor and showed anti-androgenic activity toward the androgen-dependent SC-3 cell line. Two compounds also exhibited partial agonistic activity in SC-3 assay. The docking studies of carborane derivatives to AR demonstrate that ten-vertex carborane is useful for development of novel bioactive compounds as well as twelve-vertex carboranes that are well known to be versatile pharmacophores. Ten-vertex carborane, which has not previously been applied in the field of medicinal chemistry, appears to have potential as a hydrophobic pharmacophore with characteristic properties.

Graphical abstract: Development of androgen receptor ligands by application of ten-vertex para-carborane as a novel hydrophobic core structure

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Publication details

The article was received on 28 Nov 2011, accepted on 01 Apr 2012 and first published on 03 Apr 2012


Article type: Concise Article
DOI: 10.1039/C2MD00294A
Med. Chem. Commun., 2012,3, 680-684

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    Development of androgen receptor ligands by application of ten-vertex para-carborane as a novel hydrophobic core structure

    S. Fujii, K. Ohta, T. Goto, A. Oda, H. Masuno, Y. Endo and H. Kagechika, Med. Chem. Commun., 2012, 3, 680
    DOI: 10.1039/C2MD00294A

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