Non-steroidal CYP17A1 Inhibitors: Discovery and Assessment

Tomasz M. Wróbel*, Flemming Steen Jørgensen, Amit V. Pandey, Angelika Grudzińska, Katyayani Sharma, Jibira Yakubu, Fredrik Björkling

*Corresponding author for this work

Research output: Contribution to journalReviewResearchpeer-review

14 Citations (Scopus)
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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.

Original languageEnglish
JournalJournal of Medicinal Chemistry
Volume66
Issue number10
Pages (from-to)6542–6566
ISSN0022-2623
DOIs
Publication statusPublished - 2023

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