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Structure-activity relationship of ligands of the pyrimidine nucleoside phosphorylases.
2,6-pyridinediol and 6-benzyl-2-thiouracil have been identified as being potent inhibitors of UrdPase and dThdPase respectively. Expand
Pyrimidine acyclonucleosides, inhibitors of uridine phosphorylase.
A new class of nucleoside analogs, the pyridimine acyclonucleosides, are competitive inhibitors of uridine phosphorylase but have no effect on thymicline phosphorolytic activity, and potential usage with the chemotherapeutic agent FUdR is discussed. Expand
5-benzylacyclouridine and 5-benzyloxybenzylacyclouridine, potent inhibitors of uridine phosphorylase.
These compounds are better inhibitors of uridine phosphorylase than BU, BBU, and all other compounds previously tested, and they have no effect on thymidine phosphORYlase, uridine-cytidine kinase, or thymazine kinase. Expand
Phase I clinical and pharmacological studies of benzylacyclouridine, a uridine phosphorylase inhibitor.
On the basis of this clinical study, the suggested Phase II starting dose of BAU in combination with 5-FU is 800 mg/m2 and studies combining BAU with5-FU and incorporating appropriate molecular and biochemical end points to assess the effects of this drug combination on tumor and/or surrogate tumor tissue are under way. Expand
Inhibitors of purine nucleoside phosphorylase, C(8) and C(5') substitutions.
Abstract The C(8) and C(5') positions of base and nucleoside substrates of human erythrocytic purine nucleoside phosphorylase (PNP) are promising sites for the development of an inhibitor of thisExpand
New analogues of benzylacyclouridines, specific and potent inhibitors of uridine phosphorylase from human and mouse livers.
Benzylacyclouridines, the specific inhibitors of UrdPase, and seventeen newly synthesized derivatives, modified at the pyrimidine ring, the benzyl moiety or the acyclo tail, have been tested for their potency to inhibit URDPase and thymidine phosphorylase from both human and mouse livers. Expand
Effect of the N-glycosidic bond conformation and modifications in the pentose moiety on the binding of nucleoside ligands to uridine phosphorylase.
It is concluded that the presence of a N-glycosidic bond as well as a properly oriented 3'-hydroxyl group are prerequisites for a nucleoside ligand to bind to UrdPase. Expand
Synthesis And Biological Activity Op Hydpdxymetflyl Analogs op 5-Benzylacyclouridine and 5-Benzyloxybenzylacycloaridine
Abstract Hydroxymethyl analogs of 5-benzylacyclouridine (BAU) and 5-benzyloxybenzylacyclouridine (BBAU) were synthesized by the condensation of appropriately blocked 2-(chloromethyl)glycerols withExpand
Potentiation of 5-fluoro-2'-deoxyuridine antineoplastic activity by the uridine phosphorylase inhibitors benzylacyclouridine and benzyloxybenzylacyclouridine.
At a nontoxic dose (50 microM), the two potent uridine phosphorylase inhibitors, benzylacyclouridine and BBAU, potentiated 5-fluoro-2'-deoxyuridine (FdUrd) growth inhibition of human pancreatic carcinoma and, to a lesser extent, human lung carcinoma (LX-1) cells in culture. Expand