SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug that cross-links DNA and exerts highly potent antitumor activity.

@article{Hartley2010SG2285AN,
  title={SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug that cross-links DNA and exerts highly potent antitumor activity.},
  author={John A. Hartley and Anzu Hamaguchi and Marissa Coffils and Christopher R. H. Martin and Marie Suggitt and Zhizhi Chen and Stephen J Gregson and Luke Masterson and Arnaud C Tiberghien and Janet M. Hartley and Chris J Pepper and Thet Thet Lin and Christopher Fegan and David E. Thurston and Philip Howard},
  journal={Cancer research},
  year={2010},
  volume={70 17},
  pages={
          6849-58
        }
}
The pyrrolobenzodiazepines (PBD) are naturally occurring antitumor antibiotics, and a PBD dimer (SJG-136, SG2000) is in phase II trials. Many potent PBDs contain a C2-endo-exo unsaturated motif associated with the pyrrolo C-ring. The novel compound SG2202 is a PBD dimer containing this motif. SG2285 is a water-soluble prodrug of SG2202 in which two bisulfite groups inactivate the PBD N10-C11 imines. Once the bisulfites are eliminated, the imine moieties can bind covalently in the DNA minor… 

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