Thymidine phosphorylase inhibitors with a homophthalimide skeleton.
Several N-phenylhomophthalimide derivatives were prepared and their inhibitory activity on thymidine phosphorylase/ platelet-derived endothelial cell growth factor (TP/PD-ECGF) was assessed. Among them, 2-(2,6-diethylphenyl)-7-nitro-1,2,3,4-tetrahydroisoquinoline-1,3-dione (9) was found to be a more potent inhibitor than the classical inhibitor, 5-nitrouracil (1). Lineweaver-Burk plot analysis indicated that 9 shows mixed-type competitive inhibition of TP/PD-ECGF, while 1 is a competitive inhibitor.
Kita
T
T
Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.
Takahashi
H
H
Hashimoto
Y
Y
D016228:Endothelial Growth Factors / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D010797:Phthalimides / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013939:Thymidine Phosphorylase / Q000037:antagonists & inhibitors*; D014498:Uracil / Q000031:analogs & derivatives* / Q000494:pharmacology
D016228:Endothelial Growth Factors; D004791:Enzyme Inhibitors; D010797:Phthalimides; D014498:Uracil; C057449:5-nitrouracil; D013939:Thymidine Phosphorylase