Gregson, S.J., Howard, P.W., Barcella, S., Nakamya, A., Jenkins, T.C., Kelland, L.R. and Thurston, D.E. (2000) Effect of C2/C3-endo unsaturation on the cytotoxicity and DNA-binding reactivity of pyrrolo[2,1-c][1,4]benzodiazepines. Bioorganic and Medicinal Chemistry Letters, 10 (16). pp. 1849-1851. 10.1016/S0960-894X(00)00350-4.
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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.
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry|
|Journal or Publication Title:||Bioorganic and Medicinal Chemistry Letters|
|Deposited By:||Library Staff|
|Deposited On:||09 Mar 2012 09:52|
|Last Modified:||09 Mar 2012 09:52|
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