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Novel C8-linked pyrrolobenzodiazepine (PBD)-heterocycle conjugates that recognize DNA sequences containing an inverted CCAAT box |
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| Authors: | Brucoli Federico Hawkins Rachel M James Colin H Wells Geoff Jenkins Terence C Ellis Tom Hartley John A Howard Philip W Thurston David E |
| Institution: | a The School of Pharmacy, University of London, London WC1N 1AX, UK b University of Greenwich, Chatham, Kent ME4 4TB, UK c University College London, London WC1E 6BT, UK d Spirogen Ltd, 29-39 Brunswick Square, London WC1N 1AX, UK |
| 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 IIα promoter than the known C8-bis-pyrrole PBD conjugate GWL-78 (1b). |
| Keywords: | Pyrrolobenzodiazepine (PBD)-conjugate Inverted CCAAT box Nuclear Factor Y Topoisomerase IIα Anticancer agents |
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