Rational drug design for the treatment of hormone refractory prostate cancer

CARB 2

Michael E. Jung, jung@chem.ucla.edu, Department of Chemistry and Biochemistry, UCLA, 405 Hilgard Avenue, Los Angeles, CA 90095-1569
The switch from hormone sensitive to hormone refractory prostate cancer involves the upregulation of the androgen receptor (AR). Therefore to effectively treat hormone refractory prostate cancer, one would require much more potent androgen receptor antagonists than the ones currently available. A new class of potent androgen receptor antagonists was designed and prepared. Biological data shows that these compounds are extremely effective at inhibiting the growth of prostate cancer cells in which the AR has been overexpressed. A summary of the design, preparation, and biological testing of these new AR antagonists will be presented.