Design of a Composite Ethidium–Netropsin–Anilinoacridine Molecule for DNA Recognition (pages 50–61)
Carolina Carrasco, Philippe Helissey, Michelyne Haroun, Brigitte Baldeyrou, Amélie Lansiaux, Pierre Colson, Claude Houssier, Sylviane Giorgi-Renault and Christian Bailly
Article first published online: 3 JAN 2003 | DOI: 10.1002/cbic.200390014
Ganging up on tumors: The new trifunctional DNA ligand R-132 (shown in the picture) combines a central bispyrrole unit, which mimics the antibiotic netropsin, with two intercalating chromophores, ethidium and anilinoacridine, positioned at both ends. The three moieties of the combilexin molecule interact with DNA through a concerted intercalation and minor groove-binding mode. R-132 is a potent poison of DNA topoisomerase II and displays cytotoxic activities. It therefore provides a lead for the design of gene-targeted antitumor agents.