Publication | Open Access
Discovery of Novel Non-Steroidal Cytochrome P450 17A1 Inhibitors as Potential Prostate Cancer Agents
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Citations
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References
2020
Year
Sub µMPharmacotherapyChemical BiologyPharmaceutical ChemistryMolecular PharmacologyMedicinal ChemistryKey EnzymeAnti-cancer AgentSteroid MetabolismCancer ResearchBiochemistryAromataseProstatic DiseaseDrug DevelopmentPharmacologyUrologyNatural SciencesMedicineDrug Discovery
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.
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