(o-and p-nitrobenzyloxycarbonyl)-5-fluorouracil derivatives as potential conjugated bioreductive alkylating agents

…, L Wang, I Antonini, LA Cosby, DA Shiba…

Index: Lin, Tai-Shun; Wang, Lin; Antonini, Ippolito; Cosby, Lucille A.; Shiba, David A.; et al. Journal of Medicinal Chemistry, 1986 , vol. 29, # 1 p. 84 - 89

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Citation Number: 13

Abstract

A series of (0-and p-nitrobenzyloxycarbnyl)-5-fluorouracil derivatives were synthesized by reacting o-or p-nitrobenzyl chloroformate with 5-fluorouracil in the presence of triethylamine in DMF or Me2S0. The reductive activation of these agents was hypothesized to generate a reactive methide and &fluorouracil, two components that are capable of synergistic interaction through complementary inhibition. Measurement of the surviving fractions of ...