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Synthesis, biophysical studies, and antiproliferative activity of platinum(II) complexes having 1,2-bis(aminomethyl)carbobicyclic ligands
Mier-Vinue J de, M Gay, AM Montana, RI Saez, V Moreno, J Kasparkova, O Vrana, P Heringova, V Brabec, A Boccarelli, M Coluccia, G Natile
Jazyk angličtina Země Spojené státy americké
Typ dokumentu práce podpořená grantem
Grantová podpora
NR8562
MZ0
CEP - Centrální evidence projektů
PubMed
18197615
Knihovny.cz E-zdroje
- MeSH
- adukty DNA chemie MeSH
- chelátory chemická syntéza chemie MeSH
- chemorezistence MeSH
- cisplatina farmakologie MeSH
- diaminy * farmakologie chemická syntéza chemie MeSH
- DNA chemie MeSH
- glutathion chemie MeSH
- kinetika MeSH
- lidé MeSH
- ligandy MeSH
- můstkové bicyklické sloučeniny * farmakologie chemická syntéza chemie MeSH
- nádorové buněčné linie MeSH
- platina * MeSH
- protinádorové látky * farmakologie chemická syntéza chemie MeSH
- reagencia zkříženě vázaná chemická syntéza chemie MeSH
- screeningové testy protinádorových léčiv MeSH
- tranzitní teplota MeSH
- Check Tag
- lidé MeSH
- ženské pohlaví MeSH
- Publikační typ
- práce podpořená grantem MeSH
A selected chemical library of six platinum(II) complexes having 1,2-bis(aminomethyl)carbobicyclic ligands were synthesized after a rational design in order to evaluate their antiproliferative activity and the structure-activity relationships. The cytotoxicity studies were performed using cancer cell lines sensitive (A2780) and resistant (A2780R) to cisplatin. Excellent cytotoxicity was observed for most of complexes, which presented better resistance factors than cisplatin against the A2780R cell line. The interaction of these complexes with DNA, as the target biomolecule, was evaluated by several methods: DNA-platinum binding kinetics, changes in the DNA melting temperature, evaluation of the unwinding angle of supercoiled DNA, evaluation of the interstrand cross-links, and replication mapping. The kinetics of the interaction with glutathione was also investigated to better understand the resistant factors observed for the new complexes.
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- $a A selected chemical library of six platinum(II) complexes having 1,2-bis(aminomethyl)carbobicyclic ligands were synthesized after a rational design in order to evaluate their antiproliferative activity and the structure-activity relationships. The cytotoxicity studies were performed using cancer cell lines sensitive (A2780) and resistant (A2780R) to cisplatin. Excellent cytotoxicity was observed for most of complexes, which presented better resistance factors than cisplatin against the A2780R cell line. The interaction of these complexes with DNA, as the target biomolecule, was evaluated by several methods: DNA-platinum binding kinetics, changes in the DNA melting temperature, evaluation of the unwinding angle of supercoiled DNA, evaluation of the interstrand cross-links, and replication mapping. The kinetics of the interaction with glutathione was also investigated to better understand the resistant factors observed for the new complexes.
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