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DNA minor groove interactions and the biological activity of 2,5-bis
1CRC Biomolecular Structure Unit, Chester Beatty Laboratories, The Institute of Cancer Research, London, UK.
Bioorganic & Medicinal Chemistry Letters
|December 29, 2000
Abstract:
2,5-Bis-[4-(N-cyclobutyl-amidino)phenyl] furan and 2,5-bis-[4-(N-cyclohexyl-amidino)phenyl] furan have activity against Pneumocystis carinii and also show cytotoxicity against several tumour cell lines. These activities are correlated with DNA-binding abilities; the crystal structures of complexes with the DNA sequence d(CGCGAATTCGCG) is reported here. Interactions with, and effects on, the DNA minor groove, are found to be factors in the biological properties of these compounds.