Synthesis and characterisation of metallopolyamide complexes
摘要:
Platinum(II) and ruthenium(II)-based complexes that contain imidazole, pyrrole and beta-alanine subunits, capable of recognising specific DNA base-pair sequences, have been synthesised. These polyamides, two platinum(II), [Cl(NH3)(2)Pt-L-6-beta-Ala-Py-L-4-Im](+) (HSP-2), and [Cl(NH3)(2)Pt-L-6-beta-Ala-PyPyPy-L-4-ImImIm](+) (HSP-6) and two ruthenium, Delta and Lambda-[beta-Ala-Py-L-4-Im-beta-dpq-Ru(phen)(2)](2+) (Delta and Lambda-RUP1), were designed to recognise DNA sequences up to seven base-pairs in length. They were obtained in good yield by a combination of solid and solution phase chemistries. The chirality of the ruthenium precursors Delta- and Lambda-[Ru(phen)(2)(phendo)](2+) was conserved throughout the synthesis. Characterisation was achieved using NMR, UV-Vis and ESI-MS and CD for Delta- and Lambda-RUP1. Cytotoxicity was not determined for HSP-2 or HSP-6, due to insolubility, however the IC50 values of Delta and Lambda-RUP1 were confirmed to be greater than 40 mu M (at an incubation time of 48 h). LD studies indicated that the ruthenium complexes interact with ct-DNA through a mixed binding mode, which is influenced by complex concentration and chirality. (C) 2012 Elsevier B. V. All rights reserved.
Synthesis and characterisation of metallopolyamide complexes
摘要:
Platinum(II) and ruthenium(II)-based complexes that contain imidazole, pyrrole and beta-alanine subunits, capable of recognising specific DNA base-pair sequences, have been synthesised. These polyamides, two platinum(II), [Cl(NH3)(2)Pt-L-6-beta-Ala-Py-L-4-Im](+) (HSP-2), and [Cl(NH3)(2)Pt-L-6-beta-Ala-PyPyPy-L-4-ImImIm](+) (HSP-6) and two ruthenium, Delta and Lambda-[beta-Ala-Py-L-4-Im-beta-dpq-Ru(phen)(2)](2+) (Delta and Lambda-RUP1), were designed to recognise DNA sequences up to seven base-pairs in length. They were obtained in good yield by a combination of solid and solution phase chemistries. The chirality of the ruthenium precursors Delta- and Lambda-[Ru(phen)(2)(phendo)](2+) was conserved throughout the synthesis. Characterisation was achieved using NMR, UV-Vis and ESI-MS and CD for Delta- and Lambda-RUP1. Cytotoxicity was not determined for HSP-2 or HSP-6, due to insolubility, however the IC50 values of Delta and Lambda-RUP1 were confirmed to be greater than 40 mu M (at an incubation time of 48 h). LD studies indicated that the ruthenium complexes interact with ct-DNA through a mixed binding mode, which is influenced by complex concentration and chirality. (C) 2012 Elsevier B. V. All rights reserved.