7‐Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase
Balzarini J., Gamboa AE., Esnouf R., Liekens S., Neyts J., De Clercq E., Camarasa M-J., Pérez-Pérez M-J.
7‐Deazaxanthine (7DX) was identified as a novel inhibitor of thymidine (dThd) phosphorylase (TPase). It inhibited the TPase reaction in a concentration‐dependent manner. At 1 mM, it almost completely prevented the TPase‐catalysed hydrolysis of dThd to thymine. The 50% inhibitory concentration (IC50) of 7DX was 40 μM in the presence of 100 μM of the natural substrate dThd. 7DX is also endowed with a marked inhibitory effect on angiogenesis. It significantly prevents neovascularisation in the chicken chorioallantoic membrane during development. 7DX is the first purine derivative shown to be a potent inhibitor of purified TPase and angiogenesis.