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New ferrocene containing peptide conjugates: Synthesis and effect on human leukemia (HL‐60) cells
Author(s) -
Miklán Zsanett,
Szabó Rita,
ZsoldosMády Virág,
Reményi Judit,
Bánóczi Zoltán,
Hudecz Ferenc
Publication year - 2007
Publication title -
peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.556
H-Index - 125
eISSN - 1097-0282
pISSN - 0006-3525
DOI - 10.1002/bip.20696
Subject(s) - chemistry , moiety , conjugate , in vitro , peptide , oligopeptide , solubility , combinatorial chemistry , leukemia , ferrocene , mtt assay , biochemistry , stereochemistry , organic chemistry , mathematical analysis , mathematics , electrode , electrochemistry , medicine
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 ferrocenylacrylic acid in solution. The antitumor effect of conjugates was analyzed by MTT assay in vitro. We demonstrated that ferrocenylacrylic acid possessing an enone (CHCHCO) 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. © 2007 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 88: 108–114, 2007. This article was originally published online as an accepted preprint. The ‘Published Online’ date corresponds to the preprint version. You can request a copy of the preprint by emailing the Biopolymers editorial office at biopolymers@wiley.com