DNA minor groove interactions and the biological activity of 2,5-bis-[4-(N-alkylamidino)phenyl] furans

Authors
Simpson, IJ Lee, M Kumar, A Boykin, DW Neidle, S
Citation
Ij. Simpson et al., DNA minor groove interactions and the biological activity of 2,5-bis-[4-(N-alkylamidino)phenyl] furans, BIOORG MED, 10(23), 2000, pp. 2593-2597
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
23
Year of publication
2000
Pages
2593 - 2597
Database
ISI
SICI code
0960-894X(200012)10:23<2593:DMGIAT>2.0.ZU;2-C
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 c orrelated with DNA-binding abilities; the crystal structures of complexes w ith the DNA sequence d(CGCGAATTCGCG) is reported here. Interactions with, a nd effects on, the DNA minor groove, are found to be factors in the biologi cal properties of these compounds. (C) 2000 Elsevier Science Ltd. All right s reserved.