A novel approach to the synthesis of cytotoxic C2-C3 unsaturated pyrrolo[2,1-c]benzodiazepines (PBDs) with conjugated acrylyl C2-substituents.

Chen, Z., Gregson, S.J., Howard, P.W. and Thurston, D.E. (2004) A novel approach to the synthesis of cytotoxic C2-C3 unsaturated pyrrolo[2,1-c]benzodiazepines (PBDs) with conjugated acrylyl C2-substituents. Bioorganic & Medicinal Chemistry Letters, 14 (6). pp. 1547-1549. 10.1016/j.bmcl.2003.12.094.

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DOI: 10.1016/j.bmcl.2003.12.094

Abstract

A concise synthesis of three novel C2-C3 unsaturated pyrrolo[2,1-c][1,4]benzodiazepine analogues (18-20) containing conjugated acrylyl C2-substituents is reported that utilises Heck coupling to install the C2-acrylyl side chains. These analogues possess significant cytotoxicity according to the NCI 60-cell line screen with 18 surpassing anthramycin (1) in potency.

Item Type:Article
Uncontrolled Keywords:Cytotoxic; DNA binding; PBDs; SAR
Departments, units and centres:Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry
ID Code:2913
Journal or Publication Title:Bioorganic & Medicinal Chemistry Letters
Deposited By:Library Staff
Deposited On:08 Mar 2012 11:26
Last Modified:08 Mar 2012 11:26

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