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

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

Brucoli, Federico, Hawkins, Rachel M., James, Colin H., Wells, Geoff, Jenkins, Terrence C., Ellis, Tom, Hartley, John A., Howard, Philip W. and Thurston, David E. (2011) Novel C8-linked pyrrolobenzodiazepine (PBD)-heterocycle conjugates that recognize DNA sequences containing an inverted CCAAT box. Bioorganic & Medicinal Chemistry Letters, 21. pp. 3780-3783. ISSN 0960-894X (online) (doi:10.1016/j.bmcl.2011.04.054)

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Abstract

A series of novel DNA-interactive C8-linked pyrrolobenzodiazepine (PBD)–heterocycle polyamide 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 IIa promoter than the known C8-bis-pyrrole PBD conjugate GWL-78 (1b).

Item Type: Article
Uncontrolled Keywords: pyrrolobenzodiazepine (PBD)-conjugate, inverted CCAAT box, nuclear factor Y, topoisomerase IIa, nticancer agents
Subjects: R Medicine > RM Therapeutics. Pharmacology
R Medicine > RS Pharmacy and materia medica
Faculty / Department / Research Group: Faculty of Engineering & Science > Department of Pharmaceutical, Chemical & Environmental Sciences
Related URLs:
Last Modified: 07 Dec 2016 10:12
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
URI: http://gala.gre.ac.uk/id/eprint/7503

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