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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)

Full text not available from this repository.
Official URL: http://dx.doi.org/10.1016/j.bmcl.2011.04.054

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
School / Department / Research Groups: School of Science
School of Science > Department of Pharmaceutical, Chemical & Environmental Sciences
Related URLs:
Last Modified: 16 Feb 2012 12:59
URI: http://gala.gre.ac.uk/id/eprint/7503

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