“…The sequence selectivity of DNA modification by platinum complexes was evaluated by the primer extension footprinting assay (13,14). PBR 322 double stranded DNA (1.5x10 -8 mol nucleotides) was reacted with platinum complexes (drug/nucleotide molar ratio 0.02) in a total volume of 10 …”
The metal-coordinating properties of acyclovir are of current interest (2-5) from a mechanistic point of view, some DNA polymerases containing (Zn2+) and/or being
“…The sequence selectivity of DNA modification by platinum complexes was evaluated by the primer extension footprinting assay (13,14). PBR 322 double stranded DNA (1.5x10 -8 mol nucleotides) was reacted with platinum complexes (drug/nucleotide molar ratio 0.02) in a total volume of 10 …”
The metal-coordinating properties of acyclovir are of current interest (2-5) from a mechanistic point of view, some DNA polymerases containing (Zn2+) and/or being
“…According to the literature [15], the binuclear platinum complexes [PtLI 2 ] 2 were synthesized from the reaction of cis-[Pt(L) 2 I 2 ] (L ¼ amine) with perchloric acid. In these conditions, one amine is protonated.…”
“…Most cisplatin analogues described in the literature contain either two identical amine ligands, a chelating didentate ligand or an ammine and an amine ligand. Asymmetrical complexes with two different amine substituents coordinating in cis position present an attractive, but as yet less studied class of platinum complexes with cytotoxic potential [5][6][7][8][9][10][11]. An efficient synthetic method that could be applied for a combinatorial evaluation of this class of compounds would enable in-depth analysis leading to a better understanding of these complexes.…”
Section: Introductionmentioning
confidence: 99%
“…In solution, it is difficult to form such a mono-amine complex: in the reaction of [PtX 4 ] 2À with one equivalent of N-donating ligand there is little or no control over mono-versus disubstitution, in fact, there is even a preference to form the cis diamine species. The three-step procedure as described by Rochon et al [5] involving a bridged dinuclear intermediate is a useful method to access asymmetrical cis-diamineplatinum complexes in solution. However, this procedure is rather delicate and unsuitable for the rapid preparation of an array of asymmetric cisplatin analogues.…”
Section: Introductionmentioning
confidence: 99%
“…After characterisation, the crude complexes were subjected to a cytotoxicity screen, which revealed several complexes with activities comparable to cisplatin. Two of the more active compounds were selected and resynthesised on larger scale in solution using earlier described methods [5,10]. These two compounds were analysed in detail and their IC 50 value was determined in two different cell lines, sensitive and resistant to cisplatin.…”
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