摘要：The DNA binding properties of three novel extended diphenylfuran bisamidines (1—3) possessing different dicationic terminal side chains were studied. The ultrafiltration assay showed that bisamidines 1—3 have significant affinity for DNA. The DNA-binding data for bisamidines 1—3 using homopolymers poly(dA-dT)·poly(dA-dT) and poly(dG-dC)·poly(dG-dC), indicated that these compounds show moderate specificity for AT base pairs. We studied the cytotoxicity effects of bisamidines 1—3, Hoechst 33258 and DAPI (4',6-diamidino-2-phenylindole) in cultured breast cancer MCF-7 cells. The bisamidines 1—3 showed comparable antitumour activity to Hoechst 33258, but were substantially more cytotoxic compared to DAPI. These data show that in broad terms the cytotoxic potency of bisamidines 1—3 in cultured breast cancer MCF-7 cells decreases with the size of the alkyl group substituent (cyclopropyl>isopropyl>cyclopentyl), in accord with their increases in DNA affinity, as shown by the binding constant values.
关键词：bisamidine;DNA-binding;utrafiltration assay;breast cancer MCF-7 cells
