A C2/C2′-exo unsaturated pyrrolobenzodiazepine dimer 1 has been synthesised which is cytotoxic at the picomolar level and has remarkable covalent DNA binding affinity, raising the melting temperature of duplex-form calf thymus DNA by 34 °C after 18 h incubation.
S. J. Gregson, P. W. Howard, D. E. Thurston, T. C. Jenkins and L. R. Kelland, Chem. Commun., 1999, 797 DOI: 10.1039/A809791G
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