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
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
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