title: Synthesis and anchoring of antineoplastic ferrocene and phthalocyanine derivatives on water-soluble polymeric drug carriers derived from lysine and aspartic Acid.
abstract: The general synthetic strategy towards water-soluble biodegradable drug carriers and the properties that they must have are discussed. The syntheses of water-soluble biodegradable copolymers of lysine and aspartic acid as potential drug-delivering devices, having amine-functionalised side chains are then described. Covalent anchoring of carboxylic acid derivatives of the antineoplastic ferrocene and photodynamically active phthalocyanine moieties to the amine-containing drug carrier copolymers under mild coupling conditions has been achieved utilising the coupling reagent O-benzotriazolyl-N,N,N('),N(')-tetramethyluronium hexafluorophosphate to promote formation of the biodegradable amide bond. Even though the parent antineoplastic ferrocene and phthalocyanine derivatives are themselves insoluble in water at pH < 7, the new carrier-drug conjugates that were obtained are well water-soluble.
authors.affiliation: Department of Chemistry, University of the Free State, Bloemfontein 9300, South Africa.
authors.forename: M David
authors.initials: MD
authors.lastname: Maree
authors.forename: Eberhard W
authors.initials: EW
authors.lastname: Neuse
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Erasmus
authors.forename: Jannie C
authors.initials: JC
authors.lastname: Swarts