New ferrocene containing peptide conjugates:: Synthesis and effect on human leukemia (HL-60) cells

Data reported in this article describe the synthesis of Arg-rich oligopeptide conjugates of ferrocenecarboxylic acid on solid support with two different strategies and for the first time, the successful preparation of peptide conjugates of ferrocenylarcrylic acid in solution. The antitumor effect of conjugates was analyzed by MTT assay in vitro. We demonstrated that ferrocenylacrylic acid possessing an enone (-CH=CH-CO-) moiety exhibited remarkable antiproliferative effect against human leukemia cells (HL-60) in vitro, but its effect was not improved by conjugation with hexa- or octaarginines. However, we observed highly increased water-solubility. In contrast, the results provide evidence that conjugation of ferrocenecarboxylic acid to Arg(n) (n = 6, 8) improved not only its water solubility, but also antitumor effect on human leukemia cells in vitro. (c) 2007 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 88: 108-114, 2007.