Platinum (II) Complexes with Stereochemically-defined Thiepane Dioxide Diamine Ligands as Anticancer Drugs

Platinum (II) complexes are accredited with biological activities. New complexes with thiepane dioxide diamine as ligands, characterized by defined stereochemical features, a flexible 7-membered thiepane moiety and by C 2 symmetry, were prepared. The complexes, related to the diamino cyclohexane fam...

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Bibliographic Details
Published in:Anticancer research 2006-05, Vol.26 (3A), p.1815-1819
Main Authors: CERE, Vanda, GROSSI, Loris, MUNARI, Daniela, POLLICINO, Salvatore, MARTELLI, Laura, MARTELLI, Mario
Format: Article
Language:English
Subjects:
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Line, Tumor
Cisplatin - pharmacology
Drug Resistance, Neoplasm
Drug Screening Assays, Antitumor
Female
Humans
Ligands
Medical sciences
Organoplatinum Compounds - chemical synthesis
Organoplatinum Compounds - chemistry
Organoplatinum Compounds - pharmacology
Oxides - chemical synthesis
Oxides - chemistry
Oxides - pharmacology
Stereoisomerism
Thiepins - chemical synthesis
Thiepins - chemistry
Thiepins - pharmacology
Tumors
Uterine Cervical Neoplasms - drug therapy
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Summary:Platinum (II) complexes are accredited with biological activities. New complexes with thiepane dioxide diamine as ligands, characterized by defined stereochemical features, a flexible 7-membered thiepane moiety and by C 2 symmetry, were prepared. The complexes, related to the diamino cyclohexane family of platinum complexes, were soluble in dimethyl sulfoxide with the solvent substituting one chloride ion. These positively-charged complexes were tested against a human carcinoma cell line A431 and its cisplatin-resistant counterpart A431/Pt and were found to show: i) capability in bypassing cisplatin-resistance; ii) cytotoxicity comparable to that of oxaliplatin; iii) lower activity than cisplatin. In both cells lines, [PtCl(DACH)(DMSO)] + was more cytotoxic than oxaliplatin. The best activity was shown by the platinum complexes with ligands which presented C 2 symmetry.
ISSN:0250-7005
1791-7530