In vitro antitumour activity and cellular pharmacological properties of the platinum-iminoether complex trans-[PtCl2[E-HN=C(OMe)Me]2]. |
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| Authors: | M Coluccia A Nassi A Boccarelli D Giordano N Cardellicchio F P Intini G Natile A Barletta A Paradiso |
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| Affiliation: | Dipartimento Scienze Biomediche e Oncologia Umana, Universia di Bari, I-70124 Bari, Italy. |
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| Abstract: | The platinum complex trans-[PtCl2?E-HN=C(OMe)Me?2] was compared to cisplatin for cytotoxicity towards tumour cells, and for cellular pharmacological properties in A2780 and cisplatin-resistant A2780/Cp8 ovarian cancer cells. Trans-[PtCl2?E-HN=C(OMe)Me?2] was comparably cytotoxic to cisplatin (mean IC50 after 72 h exposure = 6. 1 microM and 7 microM, respectively) and did not show cross-resistance in A2780/Cp8 cells (resistance factor = 0.9). Cellular accumulation measurements after treatment with equimolar drug concentrations showed that trans-[PtCl2?E-HN=C(OMe)Me?2] entered both A2780 and A2780/Cp8 cells much more efficiently than cisplatin, whose accumulation was 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 cells, thus indicating substantially different mechanistic properties. |
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