Abstract:5-Fluorouracil and 5-fluorouracil-based prodrugs have
been used
clinically for decades to treat cancer. Their anticancer effects are
most prominently ascribed to inhibition of thymidylate synthase (TS)
by metabolite 5-fluoro-2′-deoxyuridine 5′-monophosphate
(FdUMP). However, 5-fluorouracil and FdUMP are subject to numerous
unfavorable metabolic events that can drive undesired systemic toxicity.
Our previous research on antiviral nucleotides suggested that substitution
at the nucleoside 5′-carbon imposes confor… Show more
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