Cis-Pt I2(NH3)2: a reappraisal
Entity
UAM. Departamento de Química InorgánicaPublisher
Royal Society of ChemistryDate
2015-07-17Citation
10.1039/c5dt01196e
Dalton Transactions 44.33 (2015): 14896-14905
ISSN
1477-9226 (print); 1477-9234 (online)DOI
10.1039/c5dt01196eFunded by
TM and LM acknowledge Beneficentia Stiftung (Vaduz), COST Action CM1105 and AIRC (IG-16049) for generous financial support. JK and VB acknowledge the support from the Czech Science Foundation (Grant 14-21053S)Editor's Version
http://dx.doi.org/10.1039/c5dt01196eSubjects
Cell culture; Cells; Diseases; Platinum compounds; QuímicaRights
© The Royal Society of Chemistry 2015Abstract
The investigation of cis-PtI2(NH3)2, the diiodido analogue of cisplatin (cisPtI2 hereafter), has been unjustly overlooked so far mainly because of old claims of pharmacological inactivity. Some recent - but still fragmentary - findings prompted us to reconsider more systematically the chemical and biological profile of cisPtI2 in comparison with cisplatin. Its solution behaviour, interactions with DNA and cytotoxic properties versus selected cancer cell lines were thus extensively analysed through a variety of biophysical and computational methods. Notably, we found that cisPtI2 is highly cytotoxic in vitro toward a few solid tumour cell lines and that its DNA platination pattern closely reproduces that of cisplatin; cisPtI2 is also shown to completely overcome resistance to cisplatin in a platinum resistant cancer cell line. The differences in the biological actions of these two Pt complexes are most likely related to slight but meaningful differences in their solution behaviour and reactivity. Overall, a very encouraging and unexpected pharmacological profile emerges for cisPtI2 with relevant implications both in terms of mechanistic knowledge and of prospective clinical application. An ab initio DFT study is also included to support the interpretation of the solution behaviour of cisPtI2 under physiological and slightly acidic pH conditions
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Google Scholar:Marzo, Tiziano
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Pillozzi, Serena
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Hrabina, Ondrej
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Kasparkova, Jana
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Brabec, Viktor
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Arcangeli, Annarosa
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Bartoli, Gianluca
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Severi, Mirko
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Lunghi, Alessandro
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Totti, Federico
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Gabbiani, Chiara
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Gómez Quiroga, Adoración
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Messori, Luigi
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