The synthesis of a series of Pt-complexes chelating diamines derived from variously substituted 2-methylaminoimidazoles was realised. The different substituents on the basic amines of the imidazole ring and of aliphatic chain were carried out with the aim of either modulating the so called ”trans-effect”, which the activation of the platinum complexes is strictly related to, or improving the lipholicity. The initial screening study about Pt-compounds cytotoxicity on different cancer cells lines revealed, among the different platinum complexes, Pt-4a as lead compound.[1] On the basis of these results in order to increase lipophilicity and the consequent solubility of Pt(II) complexes across biological membranes it was then decided to introduce at the N1 of the imidazole moiety differently-long saturated and unsaturated aliphatic chains. Moreover a comparison with Cis-platin uptake mechanism was developed by using the octapeptide Mets 7[2] as a probe to investigate the interaction of synthetised platinum compounds with the N-terminal domain of Ctr1.

New antiproliferative platinum(II) complexes based on imidazol moiety / G. Facchetti, N. Ferri, R. Gandolfi, S. Pellegrino, E. Pini, I. Rimoldi - In: BioMet 14 : XIV Pharmacobiometallics[s.l] : CIRCMSB, 2014 Oct 24. - pp. 19-19 (( Intervento presentato al 14. convegno BioMET tenutosi a Pisa nel 2014.

New antiproliferative platinum(II) complexes based on imidazol moiety

G. Facchetti
Primo
;
N. Ferri
Secondo
;
R. Gandolfi;S. Pellegrino;E. Pini
Penultimo
;
I. Rimoldi
Ultimo
2014-10-24

Abstract

The synthesis of a series of Pt-complexes chelating diamines derived from variously substituted 2-methylaminoimidazoles was realised. The different substituents on the basic amines of the imidazole ring and of aliphatic chain were carried out with the aim of either modulating the so called ”trans-effect”, which the activation of the platinum complexes is strictly related to, or improving the lipholicity. The initial screening study about Pt-compounds cytotoxicity on different cancer cells lines revealed, among the different platinum complexes, Pt-4a as lead compound.[1] On the basis of these results in order to increase lipophilicity and the consequent solubility of Pt(II) complexes across biological membranes it was then decided to introduce at the N1 of the imidazole moiety differently-long saturated and unsaturated aliphatic chains. Moreover a comparison with Cis-platin uptake mechanism was developed by using the octapeptide Mets 7[2] as a probe to investigate the interaction of synthetised platinum compounds with the N-terminal domain of Ctr1.
Settore CHIM/03 - Chimica Generale e Inorganica
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/263993
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