Masterson, L.A., Croker, S.J., Jenkins, T.C., Howard, P.W. and Thurston, D.E. (2004) Synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) C8 cyclic amine conjugates. Bioorganic & Medicinal Chemistry Letters, 14 (4). pp. 901-964. 10.1016/j.bmcl.2003.12.017.
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We report examples of a series of novel pyrrolo[2,1-c][1,4]benzodiazepine (PBD) analogues 12-15 prepared from a common functionalized building block 11 that can be conveniently synthesized on a large scale and in optically pure form. Isoindoline analogue 15 is the most cytotoxic agent in this series, has the highest DNA-binding affinity, and shows significant activity in the in vivo hollow fibre assay.
|Uncontrolled Keywords:||DNA Binding; Gene targeting; PBDs; Pyrrolobenzodiazepines; Sequence-selective|
|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 11:34|
|Last Modified:||08 Mar 2012 11:34|
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