Joonhyung Cho1, Matt L. Childers1, Celeste A. S. Regino2, Martin W. Brechbiel2, Antonio G. DiPasquale3, Arnold L. Rheingold3, Suzy V. Torti4, Frank M. Torti4, and Roy P. Planalp1. (1) University of New Hampshire, Durham, NH, (2) National Cancer Institute, NIH, Bethesda, MD, (3) University of California - San Diego, La Jolla, CA, (4) Wake Forest University Health Sciences, Winston-Salem, NC
We present coordination chemistry of a new novel hexadentate aminopyridyl chelator, namely the relationship of chelator cytotoxicity to Fe(II), Cu(II) and Zn(II) complexation and the redox activity of the complexes. This chelator is based on the cis,cis-1,3,5-triaminocyclohexane framework, and the aminopyridyl arms are substituted with MeO (tach-3-MeOpyr) at their pyridyl rings. Ligands in this family have been found to enter cultured tumor cells and bind Fe(II), Cu(II) and Zn(II). The structures of [Fe(tach-3-MeOpyr)](FeCl4) and [Cu(tach-3-MeOpyr)](ClO4)2 will be presented. The low-spin configuration Fe(II) complex has been determined by UV-Vis and 1H-NMR. X-ray crystallographic study of Fe(II) complex shows that the ligand provides an excellent octahedral coordination geometry while Cu(II) complex shows a Jahn-Teller effect. Cytotoxicities of the chelator toward cultured Hela cancer cells have been measured, and they correspond to the rate of iron-mediated oxidative dehydrogenation of the complexes. Therefore, iron-binding is an important feature of the biological action of this chelator.
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