التفاصيل البيبلوغرافية
| العنوان: |
Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy |
| المؤلفون: |
Silvia Cesarini, Ilaria Vicenti, Federica Poggialini, Silvia Filippi, Eleonora Mancin, Lia Fiaschi, Elisa De Marchi, Federica Giammarino, Chiara Vagaggini, Bruno Mattia Bizzarri, Raffaele Saladino, Elena Dreassi, Maurizio Zazzi, Lorenzo Botta |
| المصدر: |
Molecules, Vol 29, Iss 7, p 1452 (2024) |
| بيانات النشر: |
MDPI AG, 2024. |
| سنة النشر: |
2024 |
| المجموعة: |
LCC:Organic chemistry |
| مصطلحات موضوعية: |
privileged scaffold, triazines, pyrimidines, pyridines, scaffold morphing, anticancer activity, Organic chemistry, QD241-441 |
| الوصف: |
The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques that enable the modification of the chosen privileged framework and better explore the chemical space around it. In this study, two series of highly functionalized pyrimidine and pyridine derivatives were synthesized using a scaffold morphing approach consisting of triazine compounds obtained previously as antiviral agents. Newly synthesized azines were evaluated against lymphoma, hepatocarcinoma, and colon epithelial carcinoma cells, showing in five cases acceptable to good anticancer activity associated with low cytotoxicity on healthy fibroblasts. Finally, ADME in vitro studies were conducted on the best derivatives of the two series showing good passive permeability and resistance to metabolic degradation. |
| نوع الوثيقة: |
article |
| وصف الملف: |
electronic resource |
| اللغة: |
English |
| تدمد: |
1420-3049 |
| Relation: |
https://www.mdpi.com/1420-3049/29/7/1452; https://doaj.org/toc/1420-3049 |
| DOI: |
10.3390/molecules29071452 |
| URL الوصول: |
https://doaj.org/article/e3ec79e5c0fa472db93d562a43145464 |
| رقم الانضمام: |
edsdoj.3ec79e5c0fa472db93d562a43145464 |
| قاعدة البيانات: |
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