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...

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Veröffentlicht in:	Biological & pharmaceutical bulletin 2001, Vol.24(7), pp.860-862
Hauptverfasser:	KITA, Tetsuya, TAKAHASHI, Hiroyasu, HASHIMOTO, Yuichi
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Biological and medical sciences Chemotherapy Endothelial Growth Factors - pharmacology Enzyme Inhibitors - pharmacology homophthalimide inhibitor Kinetics Magnetic Resonance Spectroscopy Medical sciences Pharmacology. Drug treatments Phthalimides - chemical synthesis Phthalimides - pharmacology platelet-derived endothelial cell growth factor Structure-Activity Relationship thymidine phosphorylase Thymidine Phosphorylase - antagonists & inhibitors Uracil - analogs & derivatives Uracil - pharmacology
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Beschreibung
Zusammenfassung:	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 TP/PD-ECGF, while 1 is a competitive inhibitor.
ISSN:	0918-6158 1347-5215
DOI:	10.1248/bpb.24.860