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Novel C8-linked pyrrolobenzodiazepine (PBD)-heterocycle conjugates that recognize DNA sequences containing an inverted CCAAT box

Brucoli, F; Hawkins, RM; James, CH; Wells, G; Jenkins, TC; Ellis, T; Hartley, JA; ... Thurston, DE; + view all (2011) Novel C8-linked pyrrolobenzodiazepine (PBD)-heterocycle conjugates that recognize DNA sequences containing an inverted CCAAT box. BIOORG MED CHEM LETT , 21 (12) 3780 - 3783. 10.1016/j.bmcl.2011.04.054.

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Abstract

A series of novel DNA-interactive C8-linked pyrrolobenzodiazepine (PBD)-heterocyclepolyamide conjugates has been synthesised to explore structure/sequence-selectivity relationships. One conjugate (2d) has a greater selectivity and DNA binding affinity for inverted CCAAT sequences within the Topoisomerase II alpha promoter than the known C8-bis-pyrrole PBD conjugate GWL-78 (1b). (C) 2011 Elsevier Ltd. All rights reserved.

Type: Article
Title: Novel C8-linked pyrrolobenzodiazepine (PBD)-heterocycle conjugates that recognize DNA sequences containing an inverted CCAAT box
DOI: 10.1016/j.bmcl.2011.04.054
Keywords: Pyrrolobenzodiazepine (PBD)-conjugate, Inverted CCAAT box, Nuclear Factor Y, Topoisomerase II alpha, Anticancer agents, TOPOISOMERASE-II-ALPHA, FACTOR NF-Y, TRANSCRIPTION FACTOR, BINDING, P53, EXPRESSION, GENE
UCL classification: UCL > School of Life and Medical Sciences
UCL > School of Life and Medical Sciences > Faculty of Life Sciences
UCL > School of Life and Medical Sciences > Faculty of Life Sciences > UCL School of Pharmacy
UCL > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > School of Life and Medical Sciences > Faculty of Medical Sciences > Wolfson Institute and Cancer Institute Administration > Cancer Institute
UCL > School of Life and Medical Sciences > Faculty of Medical Sciences > Wolfson Institute and Cancer Institute Administration > Cancer Institute > Research Department of Oncology
URI: http://discovery.ucl.ac.uk/id/eprint/1311473
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