many anticancer drugs in clinical use interact with dna through intercalation, which is process that starts with the transfer of the intercalating molecule from an aqueous environment to the hydrophobic space between two adjacent dna base pairs. in general, intercalatig agents are two types: monofunctional and bifunctional. monofunctional intercalators contain one intercalating unit and bifunct...

With the goal of developing artificial nucleases for DNA hydrolysis, metal-coordinating peptides have been tethered to a DNA-intercalating rhodium complex to deliver metal ions to the sugar-phosphate backbone. The intercalator, [Rh(phi)(2)bpy']Cl(3) [phi = 9,10-phenanthrenequinone diimine; bpy' = 4-(butyric acid)-4'-methyl-2,2'-bipyridine], provides DNA binding affinity, and a metal-binding pep...

A bis-intercalator echinomycin (ECHI) and a simple intercalator [Co(phen)3]3+ were used as a novel electrochemical redox indicators to detect DNA hybridization at gold electrodes (AuE). In order to minimize the nonspecific adsorption of oligonucleotides (ODN), the thiol-derivatized oligonucleotides were immobilized onto AuE in the first step, and the exposition of AuE to 6-mercapto-1-hexanol (M...

A novel bimetallic conjugate combining a rhodium intercalator that selectively binds DNA mismatches and a reactive cis-platinum analogue that targets DNA by coordination has been prepared. The site-selectivity of the bimetallic complex in forming coordination adducts is examined using mismatched and well-matched oligonucleotides of different sequences. The results indicate that through the bifu...

Thermodynamic studies on the interactions between intercalator-neomycin conjugates and a DNA polynucleotide triplex [poly(dA).2poly(dT)] were conducted. To draw a complete picture of such interactions, naphthalene diimide-neomycin (3) and anthraquinone-neomycin (4) conjugates were synthesized and used together with two other analogues, previously synthesized pyrene-neomycin (1) and BQQ-neomycin...

An intercalator-linked macrocycle 3,6-bis(dimethylamino)-10-(6-[1,4,7-triazacyclononane]hexyl) acridinium bromide was synthesized, its copper(ii) complex was prepared, and the DNA cleavage activity of this metal complex was compared to that of the intercalator-free (Cu[9]aneN(3))(2+) complex.

DNA strand breaks produced by damaging agents such as x-ray generally stimulate poly(adenosine diphosphoribose) (ADP-R) synthesis in mammalian cells. DNA intercalating agents induce the formation of strand breaks which are unusual in that they are associated with tightly or covalently bound protein. In order to determine whether the intercalator-induced strand breaks are associated with poly-(A...

One of the important roles of a DNA sensor is the capability of detecting genetic diseases or mutations by analyzing DNA sequence. The electrochemical detection method can be simpler and cheaper than other methods available and hence this method was investigated in this paper. For a successful electrochemical detection, several aspects should be considered including chemical treatment of electr...

A novel class of DNA cleavage agents are reported that derive activity from amino acids tethered to a photoactive intercalator.

The free radical scavengers, dimethyl sulfoxide (Me2SO) and thiourea, were used to assess the role of free radicals in the production of intercalator-induced DNA breaks and cytotoxicity in mouse leukemia L1210 cells. Both agents decreased X-ray break production, and this decrease was comparable in magnitude to the degree of inhibition of X-ray-induced cell killing. By contrast, Me2SO increased ...