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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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.
|Uncontrolled Keywords:||Cytotoxic; DNA binding; PBDs; SAR|
|Departments, units and centres:||Department of Pharmaceutical and Biological Chemistry > Department of Pharmaceutical and Biological Chemistry|
|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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