Inhibition of uridine phosphorylase: synthesis and structure-activity relationships of aryl-substituted 5-benzyluracils and 1-[(2-hydroxyethoxy) methyl]-5-benzyluracils.

GF Orr, DL Musso, GE Boswell, JL Kelley…

Index: Orr; Musso; Boswell; Kelley; Joyner; Davis; Baccanari Journal of Medicinal Chemistry, 1995 , vol. 38, # 19 p. 3850 - 3856

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Citation Number: 15

Abstract

A series of l-[(2-hydroxyethoxy) methyll-5-benzyluracils were synthesized and tested for inhibition of murine liver uridine phosphorylase (UrdPase). Inhibitors of UrdPase are reported to enhance the chemotherapeutic utility of 5-fluoro-2'-deoxyuridine and 5- fluorouracil and to ameliorate zidovudine-induced anemia in animal models. We prepared a series of 5-arylsubstituted analogues of 5-benzylacyclouridine (BAU), a good inhibitor of ...

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