Design and Synthesis of Novel Androgen Receptor Antagonists with Sterically Bulky Icosahedral Carboranes
December 2005
in “
Bioorganic & medicinal chemistry
”
TLDR New compounds with carborane showed anti-androgen effects similar to flutamide.
The study reported the design and synthesis of novel androgen receptor antagonists incorporating carborane moieties, which are known for their chemical and thermal stability and hydrophobic character. Compounds 8a, 8c, and 9d demonstrated anti-androgenic activity comparable to flutamide in assays using NIH3T3 cells transfected with a human AR expression plasmid. The findings suggested that the carborane cage served as an effective hydrophobic pharmacophore for androgen receptor antagonism.
