In vitro antitumour activity and cellular pharmacological properties of the platinum-iminoether complex trans-[PtCl2{E-HN=C(OMe)Me}(2)]

Authors
Coluccia, M Nassi, A Boccarelli, A Giordano, D Cardellicchio, N Intini, FP Natile, G Barletta, A Paradiso, A
Citation
M. Coluccia et al., In vitro antitumour activity and cellular pharmacological properties of the platinum-iminoether complex trans-[PtCl2{E-HN=C(OMe)Me}(2)], INT J ONCOL, 15(5), 1999, pp. 1039-1044
Citations number
19
Categorie Soggetti
Onconogenesis & Cancer Research
Journal title
INTERNATIONAL JOURNAL OF ONCOLOGY
ISSN journal
10196439 → ACNP
Volume
15
Issue
5
Year of publication
1999
Pages
1039 - 1044
Database
ISI
SICI code
1019-6439(199911)15:5<1039:IVAAAC>2.0.ZU;2-W
Abstract
The platinum complex trans- [PtCl2{E-HN=C(OMe) Me}(2)] was compared to cisp latin for cytotoxicity towards tumour cells, and for cellular pharmacologic al properties in A2780 and cisplatin-resistant A2780/Cp8 ovarian cancer cel ls. Trans-[PtCl2{E-HN=C(OMe)Me}(2)] was comparably cytotoxic to cisplatin ( mean IC50 after 72 h exposure = 6.1 mu M and 7 mu M, respectively) and did not show cross-resistance in A2780/Cp8 cells (resistance factor = 0.9). Cel lular accumulation measurements after treatment with equimolar drug concent rations showed that trans-[PtCl2{E-HN=C(OMe) Me}(2)] entered both A2780 and A2780/Cp8 cells much more efficiently than cisplatin, whose accumulation w as reduced in A2780/Cp8 cells. Unlike cisplatin, trans-[PtCl2{E-HN=C(OMe)Me }(2)] induced rapidly cell death and cell cycle modifications of treated ce lls, thus indicating substantially different mechanistic properties.