A new class of androgen receptor antagonists bearing carborane in place of a steroidal skeleton.
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.
Fujii
Shinya
S
Faculty of Pharmaceutical Sciences at Kagawa Campus, Tokushima Bunri University, 1314-1 Shido, Sanuki 769-2193, Japan.
Hashimoto
Yuichi
Y
Suzuki
Tomoharu
T
Ohta
Shigeru
S
Endo
Yasuyuki
Y
D000726:Androgen Antagonists / Q000737:chemistry* / Q000494:pharmacology; D059002:Androgen Receptor Antagonists; D000818:Animals; D002460:Cell Line; D006860:Hydrogen Bonding; D051379:Mice; D013256:Steroids / Q000737:chemistry*
D000726:Androgen Antagonists; D059002:Androgen Receptor Antagonists; D013256:Steroids