Analytical, Diagnostic and Therapeutic Techniques and Equipment Commons^™

Preliminary Investigations Into Triazole Derived Androgen Receptor Antagonists, Jarrad Altimari, Birunthi Niranjan, Gail Risbridger, Stephanie Schweiker, Anna Lohning, Luke Henderson

Anna Lohning

A range of 1,4-substituted-1,2,3-N-phenyltriazoles were synthesized and evaluated as non-steroidal androgen receptor (AR) antagonists. The motivation for this study was to replace the N-phenyl amide portion of small molecule antiandrogens with a 1,2,3-triazole and determine effects, if any, on biological activity. The synthetic methodology presented herein is robust, high yielding and extremely rapid. Using this methodology a series of 17 N-aryl triazoles were synthesized from commercially available starting materials in less than 3 h. After preliminary biological screening at 20 and 40 lM, the most promising three compounds were found to display IC50 values of 40–50 lM against androgen dependent …