Solution behaviour and biological activity of bisamidine complexes of platinum(II)
| Autor: | Roberta Bertani, Rino A. Michelin, Roberta Seraglia, Tamás Kiss, Christine Marzano, S. Mazzega Sbovata, Alfonso Venzo, Frazia Bettio |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Spectrometry
Mass Electrospray Ionization Magnetic Resonance Spectroscopy Cell Survival Stereochemistry Electrospray ionization Amidines cisplatin chemistry.chemical_element Platinum Compounds Type (model theory) Biochemistry Benzamidine Inorganic Chemistry Amidine chemistry.chemical_compound Isomerism Cell Line Tumor Humans cisplatin cytotoxicity platinum amidine complexes drug resistance Furans platinum amidine complexes Platinum drug resistance Molecular Structure Dimethyl sulfoxide Cationic polymerization DNA amidine complexes NMR Solutions Cross-Linking Reagents chemistry cytotoxicity Derivative (chemistry) |
| Zdroj: | JBIC. Journal of biological inorganic chemistry 12 (2007): 477–493. doi:10.1007/s00775-006-0202-x info:cnr-pdr/source/autori:C. Marzano; S. Mazzega Sbovata; F. Bettio; R.A. Michelin; R. Seraglia; T. Kiss; A. Venzo; R. Bertani/titolo:Solution behaviour and biological activity of bisamidine complexes of platinum(II)/doi:10.1007%2Fs00775-006-0202-x/rivista:JBIC. Journal of biological inorganic chemistry (Print)/anno:2007/pagina_da:477/pagina_a:493/intervallo_pagine:477–493/volume:12 |
| ISSN: | 1432-1327 0949-8257 |
| DOI: | 10.1007/s00775-006-0202-x |
| Popis: | A series of platinum(II) amidine complexes were previously prepared with the aim of obtaining a new class of platinum-based antitumour drugs. This series includes compounds of the type cis-[PtCl2{Z-HN=C(NHMe)Me}2] and trans-[PtCl2{Z-HN=C(NHMe)Me}2] (1, 2 ), cis-[PtCl2{E-HN=C(NMe2)Me}2] and trans-[PtCl2{E-HN=C(NMe2)Me}2] (3 , 4), cis-[PtCl2{Z-HN=C(NHMe)Ph}2] and trans-[PtCl2{Z-HN=C(NHMe)Ph}2] (5 , 6), and cis-[PtCl2{HN=C(NMe2)Ph}2] and trans-[PtCl2{HN=C(NMe2)Ph}2] (7 , 8 ). The reactions with dimethyl sulfoxide were studied for complexes 5 - 8 ; the formation of cationic species con-taining coordinated dimethyl sulfoxide was demon-strated by NMR experiments and electrospray ionization mass spectrometry. In this work, the ami-dine platinum(II) complexes were tested for their in vitro cytotoxicity on a panel of various human cancer cell lines. The results indicate that the benzamidine complex 8 was the most effective derivative also cir-cumventing acquired cisplatin resistance as demon-strated by chemosensitivity tests performed on cisplatin-sensitive and cisplatin-resistant cell lines. The studies concerning the cellular DNA damage on both parental chemosensitive and resistant sublines suggest for the new trans-amidine complex a different mecha-nism of action compared with that exhibited by cis-platin. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|