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Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents.


ABSTRACT: The current study presents the design, synthesis, and evaluation of novel cytochrome P450 17A1 (CYP17A1) ligands. CYP17A1 is a key enzyme in the steroidogenic pathway that produces androgens among other steroids, and it is implicated in prostate cancer. The obtained compounds are potent enzyme inhibitors (sub µM) with antiproliferative activity in prostate cancer cell lines. The binding mode of these compounds is also discussed.

SUBMITTER: Wrobel TM 

PROVIDER: S-EPMC7402352 | biostudies-literature | 2020 Jul

REPOSITORIES: biostudies-literature

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Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents.

Wróbel Tomasz M TM   Rogova Oksana O   Andersen Kasper L KL   Yadav Rahul R   Brixius-Anderko Simone S   Scott Emily E EE   Olsen Lars L   Jørgensen Flemming Steen FS   Björkling Fredrik F  

International journal of molecular sciences 20200709 14


The current study presents the design, synthesis, and evaluation of novel cytochrome P450 17A1 (CYP17A1) ligands. CYP17A1 is a key enzyme in the steroidogenic pathway that produces androgens among other steroids, and it is implicated in prostate cancer. The obtained compounds are potent enzyme inhibitors (sub µM) with antiproliferative activity in prostate cancer cell lines. The binding mode of these compounds is also discussed. ...[more]

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