6533b861fe1ef96bd12c4fb2
RESEARCH PRODUCT
New propylamine oligopyrrole carboxamides linked to a heterocyclic or anthraquinone system: synthesis, DNA binding, topoisomerase I inhibition and cytotoxicity
Christian HotzelAnnalisa MarottoUlf Pindursubject
Tertiary amineStereochemistryOligonucleotidesAnthraquinonesAntineoplastic AgentsPropylamineNucleic Acid DenaturationAnthraquinoneChemical synthesischemistry.chemical_compoundDrug DiscoveryTumor Cells CulturedmedicineAnimalsHumansCytotoxicityPharmacologyPropylaminesbiologyTopoisomeraseDistamycinsOrganic ChemistryNetropsinDNAGeneral MedicineLigand (biochemistry)Intercalating AgentsMechanism of actionchemistryNetropsinbiology.proteinNucleic Acid ConformationCattleTopoisomerase I Inhibitorsmedicine.symptomDNAdescription
Continuing our studies on combilexines, compounds consisting of a DNA intercalator linked to a minor groove ligand, new results are presented. The synthesis of a series of new propylamine oligopyrrole carboxamides closely related to netropsin and distamycin A, linked to a heterocyclic or anthraquinone system is reported. The cytotoxic activity in vitro, the DNA binding characteristics and the inhibition of the topoisomerase I of the compounds were studied in order to explain the biological mechanism of action of these new potential combilexines. Some of the synthesised compounds showed cytotoxic activity against human tumour cell lines, as well as DNA binding and topoisomerase I inhibiting properties.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2003-02-01 | European Journal of Medicinal Chemistry |