Academic Journal
Synthesis and Structure-Activity Relationships of Novel Non-Steroidal CYP17A1 Inhibitors as Potential Prostate Cancer Agents.
| العنوان: | Synthesis and Structure-Activity Relationships of Novel Non-Steroidal CYP17A1 Inhibitors as Potential Prostate Cancer Agents. |
|---|---|
| المؤلفون: | Wróbel, Tomasz M, Rogova, Oksana, Sharma, Katyayani, Rojas Velazquez, Maria Natalia, Pandey, Amit Vikram, Jørgensen, Flemming Steen, Arendrup, Frederic S, Andersen, Kasper L, Björkling, Fredrik |
| المصدر: | Wróbel, Tomasz M; Rogova, Oksana; Sharma, Katyayani; Rojas Velazquez, Maria Natalia; Pandey, Amit Vikram; Jørgensen, Flemming Steen; Arendrup, Frederic S; Andersen, Kasper L; Björkling, Fredrik (2022). Synthesis and Structure-Activity Relationships of Novel Non-Steroidal CYP17A1 Inhibitors as Potential Prostate Cancer Agents. Biomolecules, 12(2) MDPI 10.3390/biom12020165 |
| بيانات النشر: | MDPI |
| سنة النشر: | 2022 |
| المجموعة: | BORIS (Bern Open Repository and Information System, University of Bern) |
| مصطلحات موضوعية: | 610 Medicine & health |
| الوصف: | Twenty new compounds, targeting CYP17A1, were synthesized, based on our previous work on a benzimidazole scaffold, and their biological activity evaluated. Inhibition of CYP17A1 is an important modality in the treatment of prostate cancer, which remains the most abundant cancer type in men. The biological assessment included CYP17A1 hydroxylase and lyase inhibition, CYP3A4 and P450 oxidoreductase (POR) inhibition, as well as antiproliferative activity in PC3 prostate cancer cells. The most potent compounds were selected for further analyses including in silico modeling. This combined effort resulted in a compound (comp 2, IC50 1.2 µM, in CYP17A1) with a potency comparable to abiraterone and selectivity towards the other targets tested. In addition, the data provided an understanding of the structure-activity relationship of this novel non-steroidal compound class. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | English |
| Relation: | https://boris.unibe.ch/166109/ |
| الاتاحة: | https://boris.unibe.ch/166109/1/biomolecules-12-00165.pdf https://boris.unibe.ch/166109/ |
| Rights: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.3FE3EA53 |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |