DNA bis-intercalators

New interest has arisen in this area within the last decade. Monobridged purines such as 4 have been prepared as potential DNA bis-intercalating agents. 

DNA Bis-intercalators are of interest since they provide greater opportunity for site-... 

Winter, S. Loeber, G. DNA-binding and fluorescence properties of the DNA bis-intercalating purple oxazole dimer POPO-1. J. Biomed. Opt. 1997, 2, 125-130. 

Rye, H. S, Yue, S, Wemmer, D. E, Quesada, M. A, Haugland, R. P, Mathies, R. A. and Glazer, A. N. (1992). Stable fluorescent complexes of double-stranded DNA with bis-intercalating asymmetric cyanine dyes -Properties and applications. Nucleic Acids Res. 20, 2803-2812. 

Nucleic acids do not display the same promiscuous chemical reactivity of proteins. Instead, individual synthetic nucleotides can display a unique functional group that can be exploited even more for direct attachment of probes (117). The simplest method of labeling DNA uses high-affinity bis-intercalating dyes such as ethidium bromide, acridine, and thiazole orange monomers... 

Intercalators have generally high DNA-binding constants (partition coefficients), and therefore after the interaction between intercalator compound and double helix, a conformational change occurs onto DNA that gives a very favorable free energy of complex formation [14], On the other hand, in bis-intercalators, for example, Echinomycin, two intercalative interactions perform via covalent bonds between aromatic rings of the molecule and DNA [14]. 

Some other examples about drug-DNA interactions have been seen in the literature. The antibiotic mitomycin C (MC) and its interactions with DNA were investgated based on guanine oxidation signal by Ozkan et al [78]. Meric et al [53] described a biosensor for the detection of interaction between a compound synthesized as an alkylating anticancer agent and DNA. Jelen et al [79] found a redox active bis-intercalator anticancer drug, Echinomycin, and they showed its interactions with DNA. The intercalator "Adriamycin" and its in situ interaction with DNA was reported by Brett et al [80]. 

Y. Chu, V. Lynch, B. L. Iverson, Tetrahedron 2006, 62,5536-5548. Synthesis and DNA binding studies of bis-intercalators with a novel spiro-cyclic linker. 

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