title: Enhancement of aqueous solubility and stability employing a trans acetate axis in trans planar amine platinum compounds while maintaining the biological profile.
abstract: A general approach to solubilization and possible in vivo activation of the transplatinum geometry is presented. The synthesis and characterization of new water-soluble cytotoxic transplatinum compounds are described. Use of acetate ligands (and carboxylate ligands in general) in trans-[Pt(OAc)(2)(L)(L')] results in significantly enhanced aqueous solubility and chemical stability in comparison to the parent dichlorides. The new compounds are the first cytotoxic transplatinum compounds containing an N(2)O(2) donor set, similar to carboplatin and oxaliplatin.
authors.affiliation: Department of Chemistry, Virginia Commonwealth University, Richmond, Virginia 23284-2006, USA.
authors.forename: Erin S F
authors.initials: ES
authors.lastname: Ma
authors.forename: W Douglas
authors.initials: WD
authors.lastname: Bates
authors.forename: Armistead
authors.initials: A
authors.lastname: Edmunds
authors.forename: Lloyd R
authors.initials: LR
authors.lastname: Kelland
authors.forename: Tito
authors.initials: T
authors.lastname: Fojo
authors.forename: Nicholas
authors.initials: N
authors.lastname: Farrell
mesh_terms: D000085:Acetates / Q000737:chemistry*; D000588:Amines / Q000737:chemistry*; D000970:Antineoplastic Agents / Q000737:chemistry*; D045744:Cell Line, Tumor; D002614:Chelating Agents / Q000737:chemistry*; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006868:Hydrolysis; D009944:Organoplatinum Compounds / Q000737:chemistry*; D012995:Solubility; D013329:Structure-Activity Relationship; D014867:Water
chemical_list: D000085:Acetates; D000588:Amines; D000970:Antineoplastic Agents; D002614:Chelating Agents; D009944:Organoplatinum Compounds; D014867:Water