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

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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DOI: 10.1016/S0960-894X(00)00350-4

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.

Item Type:Article
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:2925
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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