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Updated: Aug 14, 2026

Nucleoside Triphosphates - From Synthesis to Biochemical Characterization
Published on: April 3, 2014
Synthesis and DNA interaction of a mixed proflavine-phenanthroline Tröger base
Brigitte Baldeyrou1, Christelle Tardy, Christian Bailly
1INSERM U-524 et Laboratoire de Pharmacologie antitumorale du Centre Oscar Lambret, Institut de Recherches sur le Cancer, Place de Verdun, F-59045 Lille, France.
Abstract:
We report the synthesis of an asymmetric Tröger base containing the two well characterised DNA binding chromophores, proflavine and phenanthroline. The mode of interaction of the hybrid molecule was investigated by circular and linear dichroism experiments and a biochemical assay using DNA topoisomerase I. The data are compatible with a model in which the proflavine moiety intercalates between DNA base pairs and the phenanthroline ring occupies the DNA groove. DNase I cleavage experiments were carried out to investigate the sequence preference of the hybrid ligand and a well resolved footprint was detected at a site encompassing two adjacent 5'-GTC.5-GAC triplets. The sequence preference of the asymmetric molecule is compared to that of the symmetric analogues.
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