Drug intelligence / Profile preview

5FUMeOBut

Development stage
Preclinical
Lead developer
Western Sydney University
Modality
Small Molecules
01

Overview

5FUMeOBut is a synthetic derivative of the antimetabolite 5-fluorouracil (5-FU) designed to function as an axial ligand in the development of multi-mechanistic platinum(IV) prodrugs, such as PtIVP-5FUMeOBut and PtIV56-5FUMeOBut. Chemically, it consists of a 5-fluorouracil moiety linked via a methoxy spacer to a butyrate group. This modification allows for the coordination of the 5-FU derivative to a platinum(IV) center, creating a dual-action chemotherapeutic agent intended to remain inert in systemic circulation. Upon bioreductive activation within the reducing environment of cancer cells, the platinum(IV) complex releases the cytotoxic platinum(II) species and the 5FUMeOBut ligand. The released 5FUMeOBut acts as a prodrug of 5-FU, which inhibits thymidylate synthase and incorporates into RNA and DNA, thereby disrupting nucleic acid synthesis. This strategy is primarily investigated for its potential to treat cisplatin-resistant colorectal cancer by combining DNA-damaging platinum cytotoxicity with the antimetabolite effects of 5-FU.

Other names
4-((5-fluoro-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)butanoic acid5-fluorouracil-1-yl-methoxy-butyrate
02

Targets

DNATS (Thymidylate synthase)

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