J. Parrick et al., TARGETING RADIOSENSITIZERS TO DNA BY MINOR-GROOVE BINDING - NITROARENES BASED ON NETROPSIN AND DISTAMYCIN, Bioorganic & medicinal chemistry letters, 3(8), 1993, pp. 1697-1702
Four analogues of the antitumour antibiotics, netropsin and distamycin
, containing 2-nitroimidazole or 5-nitrofuran moieties were synthesise
d. All showed high affinity for DNA, including compounds with only one
pyrrole/amidine moiety, but the radiosensitizing efficiencies were po
or. The results have implications both for minor groove targeting and
the design of radiosensitizers.