Details

Autor(en) / Beteiligte

• Cesarini, Silvia
• Vicenti, Ilaria
• Poggialini, Federica
• Filippi, Silvia
• Mancin, Eleonora
• Fiaschi, Lia
• De Marchi, Elisa
• Giammarino, Federica
• Vagaggini, Chiara
• Bizzarri, Bruno Mattia
• Saladino, Raffaele
• Dreassi, Elena
• Zazzi, Maurizio
• Botta, Lorenzo

Titel

Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy

Ist Teil von

• Molecules (Basel, Switzerland), 2024-04, Vol.29 (7), p.1452

Ort / Verlag

Switzerland: MDPI AG

Erscheinungsjahr

2024

Link zum Volltext

Quelle

Free E-Journal (出版社公開部分のみ）

Beschreibungen/Notizen

• 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.