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ID: ALA1133277

Journal: Bioorg Med Chem Lett

Title: 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.

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 that the presence of C2/C3-endo unsaturation in the PBD C-ring enhances both DNA-binding reactivity and in vitro cytotoxic potency.

CiteXplore: 10969983

DOI: 10.1016/s0960-894x(00)00350-4