6533b7d9fe1ef96bd126b8d9
RESEARCH PRODUCT
cis-Dichloroplatinum(II) complexes tethered to dibenzo[c,h][1,6]naphthyridin-6-ones: Synthesis and cytotoxicity in human cancer cell lines in vitro
Johnny MorettoDavid PertuitNicolas DesboisClaire CachiaFlorence BouyerBruno Chauffertsubject
Organoplatinum Compoundsmedicine.drug_classStereochemistryAntineoplastic AgentsStructure-Activity RelationshipCell Line TumorDrug DiscoverymedicineHumansCytotoxic T cellMoleculeNaphthyridinesCytotoxicityCell ProliferationPharmacologyCisplatinDose-Response Relationship DrugMolecular StructureChemistryOrganic ChemistryGeneral MedicineHCT116 CellsIn vitroOxaliplatinCell cultureDrug Screening Assays AntitumorHT29 CellsTopoisomerase inhibitormedicine.drugdescription
A novel family of cisplatin-type complexes tethered to dibenzo[c,h][1,6]naphthyridin-6-one topoisomerase inhibitor via a polymethylene chain and their nonplatinated counterparts were prepared. Their potential cytotoxicity was assessed in three human colorectal cancer cell lines HCT 116, SW480 and HT-29 and compared to the reference molecules cisplatin and oxaliplatin. Platinated compounds were poorly active whilst nonplatinated dibenzo[c,h][1,6]naphthyridin-6-one moieties exhibited higher cytotoxic properties than cisplatin and oxaliplatin whatever the length of the polymethylene chain; molecules containing the tri- and hexamethylene chain length were the most cytotoxic.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2013-11-01 | European Journal of Medicinal Chemistry |