Prostate cancer is the second leading cause of death in American male population. Androgen molecules, through the androgen receptor, affect the normal development and maintenance of the prostate. Androgen ablation is a common therapy for prostate cancer, often through the subminitration of androgen receptor antagonists. Unfortunately prolonged exposure to anti-androgens initiates mechanisms of resistance which render treatment ineffective. To respond to the urgent need for novel anti-androgen therapies, we have developed a new class of small molecules containing the triazole moiety, which inhibit prostate spefic androgen production in prostate cancer cell lines LNCaP. Herein we will discuss our findings on the synthesis and SAR of a novel scaffold inspired by the structure of bicalutamide.

Synthesis and the biological evaluation of triazole-based novel antiandrogens

245th National Meeting (2013)

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