DNA minor groove interactions and the biological activity of 2,5-bis.
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.
Simpson
I J
IJ
CRC Biomolecular Structure Unit, Chester Beatty Laboratories, The Institute of Cancer Research, London, UK.
Lee
M
M
Kumar
A
A
Boykin
D W
DW
Neidle
S
S
D002460:Cell Line; D004247:DNA / Q000737:chemistry / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D005663:Furans / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D011010:Pneumocystis / Q000187:drug effects; D014407:Tumor Cells, Cultured
D005663:Furans; D004247:DNA