Effect of C2/C3-endo unsaturation on the cytotoxicity and DNA-binding reactivity of pyrrolo[2,1-c][1,4]benzodiazepines

Authors
Gregson, SJ Howard, PW Barcella, S Nakamya, A Jenkins, TC Kelland, LR Thurston, DE
Citation
Sj. Gregson et al., Effect of C2/C3-endo unsaturation on the cytotoxicity and DNA-binding reactivity of pyrrolo[2,1-c][1,4]benzodiazepines, BIOORG MED, 10(16), 2000, pp. 1849-1851
Citations number
10
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
16
Year of publication
2000
Pages
1849 - 1851
Database
ISI
SICI code
0960-894X(20000821)10:16<1849:EOCUOT>2.0.ZU;2-C
Abstract
A series of novel C2/C3-endo unsaturated pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) has been synthesised via cleavage of the N10-Alloc protecting group from appropriate precursors. Biophysical and biological evaluations show t hat the presence of C2/C3-endo unsaturation ill the PBD C-ring enhances bot h DNA-binding reactivity and in vitro cytotoxic potency. (C) 2000 Elsevier Science Ltd. All rights reserved.