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  • Title: A new class of androgen receptor antagonists bearing carborane in place of a steroidal skeleton.
    Author: Fujii S, Hashimoto Y, Suzuki T, Ohta S, Endo Y.
    Journal: Bioorg Med Chem Lett; 2005 Jan 03; 15(1):227-30. PubMed ID: 15582444.
    Abstract:
    A new class of androgen receptor antagonists containing dicarba-closo-dodecaborane (carborane) as a hydrophobic skeletal structure is described. The designed molecules bear the characteristic polar components of endogenous agonists, but have a hydrophobic carborane cage instead of the steroidal skeleton. These compounds bind to androgen receptor and show anti-androgenic activity towards androgen-dependent SC-3 cells with almost the same potency as the known anti-androgen hydroxyflutamide.
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