Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment

Overview

Journal J Med Chem

Publisher American Chemical Society

Specialty Chemistry

Date 2023 May 16

PMID 37191389

Authors

Tomasz M Wrobel

Flemming Steen Jorgensen

Amit V Pandey

Angelika Grudzinska

Katyayani Sharma

Jibira Yakubu

Fredrik Bjorkling

Affiliations

Soon will be listed here.

Abstract

CYP17A1 is an enzyme that plays a major role in steroidogenesis and is critically involved in the biosynthesis of steroid hormones. Therefore, it remains an attractive target in several serious hormone-dependent cancer diseases, such as prostate cancer and breast cancer. The medicinal chemistry community has been committed to the discovery and development of CYP17A1 inhibitors for many years, particularly for the treatment of castration-resistant prostate cancer. The current Perspective reflects upon the discovery and evaluation of non-steroidal CYP17A1 inhibitors from a medicinal chemistry angle. Emphasis is placed on the structural aspects of the target, key learnings from the presented chemotypes, and design guidelines for future inhibitors.

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