Title of article :
Effect of C2/C3-endo unsaturation on the cytotoxicity and dna-binding reactivity of pyrrolo[2,1-c][1,4]benzodiazepines
Author/Authors :
Stephen J. Gregson، نويسنده , , Philip W. Howard، نويسنده , , Simona Barcella، نويسنده , , Anthonia Nakamya، نويسنده , , Terence C. Jenkins، نويسنده , , Lloyd R. Kelland، نويسنده , , David E. Thurston، نويسنده ,
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.
