title: Study of the anticancer properties of tin(IV) carboxylate complexes on a panel of human tumor cell lines.
abstract: A group of organotin(IV) complexes were prepared: [SnCy3 (DMNI)] (1), [SnCy3 (BZDO)] (2), [SnCy3 (DMFU)] (3), and [SnPh2 (BZDO)2 ] (4), for which DMNIH=2,6-dimethoxynicotinic acid, BZDOH=1,4-benzodioxane-6-carboxylic acid, and DMFUH=2,5-dimethyl-3-furoic acid. The cytotoxic activities of compounds 1-4 were tested against pancreatic carcinoma (PANC-1), erythroleukemia (K562), and two glioblastoma multiform (U87 and LN-229) human cell lines; they show very high antiproliferative activity, with IC50 values in the 150-700 nM range after incubation for 72 h. Distribution of cellular DNA upon treatment with 1-4 revealed that whereas compounds 1-3 induce apoptosis in most of the cell lines, compound 4 does not affect cell viability in any cell line tested, indicating a possible difference in cytotoxic mechanism. Studies with the daunomycin-resistant K562/R cell line expressing P-glycoprotein (Pgp) showed that compounds 1-4 are not substrates of this protein efflux pump, indicating that these compounds do not induce acquisition of multidrug resistance, which is associated with the overexpression of Pgp.
authors.affiliation: Instituto de Biología Molecular y Celular, Universidad Miguel Hernández de Elche, Avenida de la Universidad s/n, 03202 Elche, Alicante, Spain.
authors.forename: Lourdes
authors.initials: L
authors.lastname: Rocamora-Reverte
authors.forename: Estefanía
authors.initials: E
authors.lastname: Carrasco-García
authors.forename: Jesús
authors.initials: J
authors.lastname: Ceballos-Torres
authors.forename: Sanjiv
authors.initials: S
authors.lastname: Prashar
authors.forename: Goran N
authors.initials: GN
authors.lastname: Kaluđerović
authors.forename: José A
authors.initials: JA
authors.lastname: Ferragut
authors.forename: Santiago
authors.initials: S
authors.lastname: Gómez-Ruiz
mesh_terms: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000378:metabolism; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002264:Carboxylic Acids / Q000737:chemistry*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008968:Molecular Conformation; D014001:Tin / Q000737:chemistry*
chemical_list: D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D056831:Coordination Complexes; D014001:Tin