Tomasz M Wróbel, Katyayani Sharma, Iole Mannella, Simonetta Oliaro-Bosso, Patrycja Nieckarz, Therina Du Toit, Clarissa Daniela Voegel, Maria Natalia Rojas Velazquez, Jibira Yakubu, Anna Matveeva, Søren Therkelsen, Flemming Steen Jørgensen, Amit V Pandey, Agnese C Pippione, Marco L Lolli, Donatella Boschi, Fredrik Björkling
This study reports on the synthesis and evaluation of novel compounds replacing the nitrogen-containing heterocyclic ring on the chemical backbone structure of cytochrome P450 17α-hydroxylase/12,20-lyase (CYP17A1) inhibitors with a phenyl bearing a sulfur-based substituent. Initial screening revealed compounds with marked inhibition of CYP17A1 activity. The selectivity of compounds was thereafter determined against cytochrome P450 21-hydroxylase, cytochrome P450 3A4, and cytochrome P450 oxidoreductase...
September 5, 2023: Biomolecules