• Corpus ID: 54102206

SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug with potent antitumor activity

@article{Hartley2008SG2285AN,
  title={SG2285, a novel C2-aryl-substituted pyrrolobenzodiazepine dimer prodrug with potent antitumor activity},
  author={John A. Hartley and Christopher R. H. Martin and Anzu Hamaguchi and Marissa Coffils and Zhizhi Chen and Stephen J Gregson and Chris J Pepper and Thet Thet Lin and Christopher Fegan and David E. Thurston and Philip Howard},
  journal={Cancer Research},
  year={2008},
  volume={68},
  pages={3302-3302}
}
3302 The pyrrolobenzodiazepines (PBDs) are a family of naturally occurring antitumor antibiotics. Many of the most potent family members contain a C2-endo-exo unsaturated motif associated with the pyrrolo C-ring of the PBD. SG2202 is a PBD dimer consisting of two PBD monomer units, which retain the endo-exo unsaturation motif in the form of a C2-aryl substituent conjugated to a 2,3 double bond, joined via their C8/C8’ positions through a propyldioxy linker. SG2285 is a prodrug of SG2202 whereby… 
1 Citations
A potent anti-CD70 antibody-drug conjugate combining a dimeric pyrrolobenzodiazepine drug with site-specific conjugation technology.
TLDR
In vitro cytotoxicity experiments demonstrated that the h1F6239C-PBD was potent and immunologically specific on CD70-positive renal cell carcinoma (RCC) and non-Hodgkin lymphoma (NHL) cell lines, demonstrating that PBDs can be effectively used for antibody-targeted therapy.