Biological & Pharmaceutical Bulletin 2001-07-01

Thymidine phosphorylase inhibitors with a homophthalimide skeleton.

T Kita, H Takahashi, Y Hashimoto

Index: Biol. Pharm. Bull. 24(7) , 860-2, (2001)

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Abstract

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.