| Título: | The design and synthessis of platinum-based DNA intercalators / |
| Autores: | Paradis, Michel, 1976- |
| Fecha: | 2000 |
| Publicador: | McGill University - MCGILL |
| Fuente: |
 |
| Tipo: | Electronic Thesis or Dissertation |
| Tema: |
Chemistry, Inorganic. Chemistry, Organic. |
| Descripción: |
Over the past years, considerable attention has focused on the synthesis of small complexes that can bind and react at specific DNA sequences. This understanding of how to target DNA sites with specificity becomes important for nucleotide probing and novel chemotherapeutics. Inert and stable transition-metal complexes are already being used for this purpose. Square planar platinum (II) complexes containing an aromatic heterocyclic ligand can insert and stack between the double helix base pairs. Two known ligands, DPPZ and phi, do intercalate DNA when chelating ruthenium, rhodium, or osmium. Here are presented the syntheses of [Pt(NH3)2DPPZ](CF 3SO3)2, [Pt(en)DPPZ](CF3SO3) 2, [Pt(phen)DPPZ](CF3SO3)2, [Pt(Me 2bpy)DPPZ](CF3SO3)2, and [Pt(phendione)DPPZ](CF 3SO3)2, and the attempted syntheses of [Pt(en)phi](PF 6)2 and [Pt(phen)phi](PF6)2. The binding constants of [Pt(NH3)2DPPZ](CF3SO3) 2 and [Pt(en)DPPZ](CF3SO3)2 to calf thymus DNA have been determined. The knowledge coming from the synthetic strategy to obtain monomers has allowed the synthesis of a platinum-based dimer, [(DPPZ)Pt{DPPZ(11-11 ')DPPZ}Pt(DPPZ)](CF3SO3)4, having two intercalative DPPZ ends. We hope that this bis-intercalator will bring into close proximity two DNA strands. |
| Idioma: | en |
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