Synthesis and evaluation of novel 17-indazole androstene derivatives designed as CYP17 inhibitors

摘要

A series of novel 1H- and 2H-indazole derivatives of the commercially available dehydroepiandrosterone acetate have been synthesized and tested for inhibition of human cytochrome 17[alpha]-hydroxylase-C17,20-lyase (CYP17), androgen receptor (AR) binding affinity, and cytotoxic potential against three prostate cancer (PC) cell lines.