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

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).

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