n10-benzyl pyrrolo[2,1-c][1,4]benzodiazepine

N10-benzyl pyrrolo[2,1-c][1,4]benzodiazepine is a synthetic small molecule analogue of the pyrrolobenzodiazepine (PBD) class of antitumor antibiotics. It was developed as a non-reducible control compound by researchers at Spirogen and the University of London to investigate nitroreductase-mediated Gene-Directed Enzyme Prodrug Therapy (GDEPT). While parent PBDs are potent DNA-alkylating agents that form covalent bonds with guanine bases in the DNA minor groove, the N10-benzyl substitution sterically blocks this interaction, resulting in significantly reduced cytotoxicity. This molecule was used in preclinical in vitro studies across various cancer cell lines, including ovarian and lung cancer, to validate the self-immolative mechanism of bioreductively-activated PBD prodrugs.

Other names

N10-benzyl-protected PBDN-10-benzyl-protected PBDN 10-benzyl-protected PBDN10-benzyl PBDN-10-benzyl PBDN 10-benzyl PBD