Steroidal Inhibitors of CYP17A1 as a Template For Novel Anti-Cancer Agents Development

Abstract

This review deals with studies of researches of novel CYP17A1 steroidal inhibitors and relative compounds published over the last ten years. The review contains six chapters in which novel targets of well-known CYP17A1 inhibirors (abiraterone and galeterone), anti-cancer and anti-proliferative activities of them major metabolites and new synthetic analogs, and in addition another nitrogen-containing androstane and pregnane derivatives are considered. In the review 354 structures of novel steroid derivatives and them anti-cancer efficiency data are considered. Analysis of the literature data allows us to consider steroidal inhibitors of CYP17A1 as multi-target anti-cancer agents with high pharmacological potential.

Synthesis and evaluation of N-alkynylaminosteroids as potential CYP450 17A1 inhibitors

“…Тем не менее, данное лекарство обладает рядом серьёзных побочных эффектов, в том числе гепато-и нефротоксичностью. Для решения данной проблемы были предприняты попытки создания аналогов абиратерона, самым успешным из которых стало бензимидазольное производное галетерон, действующий одновременно на активность CYP17A1 и рецепторов андрогенов [4,5]. Несмотря на успешное прохождение I и II фаз клинических испытаний галетерона, они были прекращены.…”