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J Inorg Biochem ; 91(1): 205-11, 2002 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-12121777

RESUMO

The crystal structures, electrochemical properties and cytotoxicities of platinum(II) and platinum(IV) complexes of the multidentate ligands N-(2-hydroxyethyl)ethane-1,2-diamine (NNOH) and ethane-1,2-diamine-N,N'-diacetic acid (H(2)enda) are reported. In the platinum(II) state the NNOH and H(2)enda ligands act as bidentate ligands, coordinating through the two amine groups with the hydroxyethyl and carboxylate groups remaining uncoordinated. Oxidation with hydrogen peroxide followed by refluxing yields the ring closed Pt(IV) complexes in which the NNOH and H(2)enda ligands are deprotonated and coordinate via the two amine groups and either the deprotonated alcohol group in the case of NNO or both carboxylato groups in the case of enda. The platinum(IV) complex of NNO is 2- to 5-fold more active against a panel of cisplatin sensitive and resistant human tumour cell lines than is the platinum(II) complex, whereas in the case of enda, the reverse is true. Ring closure to occupy both axial sites apparently leads to deactivation of platinum(IV) complexes, but a single closure does not necessarily do so.


Assuntos
Antineoplásicos/química , Sobrevivência Celular/efeitos dos fármacos , Diaminas/química , Compostos Organoplatínicos/química , Antineoplásicos/farmacologia , Cristalografia por Raios X , Diaminas/farmacologia , Resistencia a Medicamentos Antineoplásicos , Eletroquímica , Humanos , Estrutura Molecular , Compostos Organoplatínicos/farmacologia , Oxirredução , Células Tumorais Cultivadas
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