Synthesis of a novel C2/C2 '-exo unsaturated pyrrolobenzodiazepine cross-linking agent with remarkable DNA binding affinity and cytotoxicity

Authors
Gregson, SJ Howard, PW Jenkins, TC Kelland, LR Thurston, DE
Citation
Sj. Gregson et al., Synthesis of a novel C2/C2 '-exo unsaturated pyrrolobenzodiazepine cross-linking agent with remarkable DNA binding affinity and cytotoxicity, CHEM COMMUN, (9), 1999, pp. 797-798
Citations number
17
Categorie Soggetti
Chemistry
Journal title
CHEMICAL COMMUNICATIONS
ISSN journal
13597345 → ACNP
Issue
9
Year of publication
1999
Pages
797 - 798
Database
ISI
SICI code
1359-7345(19990507):9<797:SOANC'>2.0.ZU;2-B
Abstract
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 thymu s DNA by 34 degrees C after 18 h incubation.