title: Dinuclear platinum complexes with biological relevance based on the 1,2-diaminocyclohexane carrier ligand.
abstract: The synthesis of bifunctional dinuclear platinum complexes, [{PtCl(dach)}(2)-mu-Y](n+)Cl(n) (1-3; Y = H(2)N(CH(2))(3)NH(2)(CH(2))(4)NH(2), H(2)N(CH(2))(6)NH(2)(CH(2))(6)NH(2), and H(2)N(CH(2))(6)NH(2)(CH(2))(2)NH(2)(CH(2))(6)NH(2), respectively; Figure 1) is reported. There was no labilization of the polyamine linker groups of the cis-1,2-diaminocyclohexane complexes in the presence of sulfur-containing species at physiological pH, in contrast to previous studies preformed on trans complexes. Metabolism reactions are somewhat dependent on the nature of the polyamine: at physiological pH, the spermidine complex 1 forms an inert (tetraamine)platinum species in which one platinum is chelated by a central and terminal amino group. The stability of cis-geometry complexes may make them viable second-generation polynuclear platinum clinical candidates.
authors.affiliation: Department of Chemistry, Virginia Commonwealth University, Richmond, Virginia 23284-2006, USA.
authors.forename: John W
authors.initials: JW
authors.lastname: Williams
authors.forename: Yun
authors.initials: Y
authors.lastname: Qu
authors.forename: Genevieve H
authors.initials: GH
authors.lastname: Bulluss
authors.forename: Eugenio
authors.initials: E
authors.lastname: Alvorado
authors.forename: Nicholas P
authors.initials: NP
authors.lastname: Farrell
mesh_terms: D002352:Carrier Proteins; D015392:Chemistry, Inorganic / Q000379:methods*; D003514:Cyclohexylamines / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D015394:Molecular Structure; D010984:Platinum / Q000737:chemistry; D017671:Platinum Compounds / Q000737:chemistry*; D013053:Spectrophotometry; D013095:Spermidine / Q000737:chemistry
chemical_list: D002352:Carrier Proteins; D003514:Cyclohexylamines; D008024:Ligands; D017671:Platinum Compounds; D010984:Platinum; C030435:1,2-cyclohexanediamine; D013095:Spermidine