Synthesis and cytotoxic activity of 4-N-carboxybutyl-5-fluorocytosyl-Arg-Gln-Trp-Arg-Arg-Trp-Trp-Gln-Arg-NH₂.

Csaba Somlai,Estela Correche,Monica Olivella,Laia Tolosa,Maria José Gomez Lechon,György Dombi,Gábor K Tóth,Botond Penke,Ricardo D Enriz

Bioorganic & Medicinal Chemistry Letters（2012）

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摘要

We report the synthesis of Arg-Gln-Trp-Arg-Arg-Trp-Trp-Gln-Arg-NH2 attached to the 4-N-carboxybutyl-5-fluorocytosine residue at the N-terminus of the peptide via peptide bond formation is reported. This compound exhibited a significant cytotoxic activity against a culture of HepG2 cells.

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关键词

5-Fluorocytosine adduct,Nonapeptide attached to 4-N-carboxybutyl-5-fluorocytosine,Cytotoxic activity,Mitochondrial dysfunction

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