Polycyclic nitrogen heterocycles as potential thymidine phosphorylase inhibitors: synthesis, biological evaluation, and molecular docking study

• Main Authors: Karen Aknin (Author), Alexis Bontemps (Author), Amaury Farce (Author), Eric Merlet (Author), Philippe Belmont (Author), Philippe Helissey (Author), Philippe Chavatte (Author), Marie-Agnès Sari (Author), Sylviane Giorgi-Renault (Author), Stéphanie Desbène-Finck (Author)
• Format: Book
• Published: Taylor & Francis Group, 2022-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

New polycyclic heterocycles were synthesised and evaluated as potential inhibitors of thymidine phosphorylase (TP). Inspired by the pharmacophoric pyrimidinedione core of the natural substrate, four series have been designed in order to interact with large empty pockets of the active site: pyrimidoq...