5-Fluorouracil is a synthetic growth inhibitor and a thymidylate synthase (TS) inhibitor. It is named as there is a fluorine atom on the 5th carbon of a uracil ring. Fluorouracil was patented in 1956 (Hoffman La-Roche). Metabolites of 5-Fluorouracil use multiple targets to slow DNA and RNA processing and therefore cell growth. The compound can inhibit human cell growth induce apoptosis and is now used as an anti-cancer agent. Derivatives of 5-Fluorouracil were isolated from the marine sponge Phakellia fusca, which is unusual since anti-cancer agents usually do not have analogs in nature.
5-Fluorouracil is sparingly soluble in water and slightly soluble in alcohol.
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|Mechanism of Action||In vivo 5-Fluorouracil is converted into active metabolites that target multiple parts of DNA and RNA synthesis including replacement of uracil and depletion of thymidine triphosphate (TTP)|
|Cancer Applications|| |
5-Fluorouracil induces varying degrees of apoptosis in colorectal cancer (CRC) cell lines (SW480, SW620, HCT116 and HT29). It induced cytotoxic effects via targeting the metabolism of RNA bases and may induce apoptosis by activating PKCδ and caspase-9 (Mhaidat at el, 2004).
Bayomi S and Al-Badr AL (1990) Analytical profile of 5-Fluorouracil. Anal. Profiles Drug Sub. 599-639. doi:10.1016/s0099-5428(08)60682-6
Mhaidat N et al (2014) 5-Fluorouracil-induced apoptosis in colorectal cancer cells is caspase-9-dependent and mediated by activation of protein kinase C-δ.” Oncol. Lett. 8(2):699-704 PMID 25013487
Xu X (2003) 5-Fluorouracil derivatives from the sponge Phakellia fusca. Med. Prod. 66 (2): 285–288 PMID 12608868