Synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) C8 cyclic amine conjugates.

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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DOI: 10.1016/j.bmcl.2003.12.017

Abstract

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.

Item Type:Article
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
ID Code:2915
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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