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

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 inhib...

Descripción completa

Detalles Bibliográficos
Autores principales: Wróbel, Tomasz M., Rogova, Oksana, Andersen, Kasper L., Yadav, Rahul, Brixius-Anderko, Simone, Scott, Emily E., Olsen, Lars, Jørgensen, Flemming Steen, Björkling, Fredrik
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7402352/
https://www.ncbi.nlm.nih.gov/pubmed/32660148
http://dx.doi.org/10.3390/ijms21144868
Descripción
Sumario: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.

Ejemplares similares