title: Synthesis and biological evaluation of new bisphosphonate-dextran conjugates targeting breast primary tumor.
abstract: Bisphosphonates (BPs) have interesting antitumor effects as well in vitro as in vivo, despite their poor bioavailability in the organism after oral ingestion. To overcome this problem and reduce drug doses and secondary effects, we report the chemical synthesis of new bioconjugates. They were built with a nitrogen-containing BP as the drug covalently coupled to the carboxymethyldextran. This polysaccharide was used as a carrier, in order to increase BP lifetime in bloodstream and to target tumor cells which have a strong affinity with dextran. The efficiency of our vectorization system was biologically proved in vitro and in vivo on mammalian carcinoma models in mice.
authors.affiliation: Université Paris 13, Sorbonne Paris Cité, Laboratoire de Chimie, Structure, Propriétés de Biomatériaux et d'Agents Thérapeutiques (CSPBAT) , CNRS UMR 7244, 74, Rue Marcel Cachin F-93017 Bobigny, France.
authors.forename: Evelyne
authors.initials: E
authors.lastname: Migianu-Griffoni
authors.forename: Imène
authors.initials: I
authors.lastname: Chebbi
authors.forename: Souad
authors.initials: S
authors.lastname: Kachbi
authors.forename: Maelle
authors.initials: M
authors.lastname: Monteil
authors.forename: Odile
authors.initials: O
authors.lastname: Sainte-Catherine
authors.forename: Frédéric
authors.initials: F
authors.lastname: Chaubet
authors.forename: Olivier
authors.initials: O
authors.lastname: Oudar
authors.forename: Marc
authors.initials: M
authors.lastname: Lecouvey
mesh_terms: D001943:Breast Neoplasms / Q000188:drug therapy*; D045744:Cell Line, Tumor; D003911:Dextrans / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D004164:Diphosphonates / Q000138:chemical synthesis / Q000737:chemistry / Q000627:therapeutic use*; D005260:Female; D006801:Humans; D008970:Molecular Weight
chemical_list: D003911:Dextrans; D004164:Diphosphonates