Abstract
The biological evaluation of carbocyclic minor groove binders 1-6 is described. The cytotoxicity of the obtained compounds was tested on MDA-MB-231 breast cancer cells. The mechanism of action of compounds 1-6 was studied employing the topoisomerase I/II inhibition assay and ethidium displacement assay using pBR322. Determination of association constants was done using calf thymus DNA, T4 coliphage DNA, poly(dA-dT)(2), and poly(dG-dC)(2). The effect of compounds 1-6 on the amidolytic activity of plasmin, trypsin, thrombin, and urokinase was also examined.
MeSH terms
-
Aniline Compounds / metabolism*
-
Aniline Compounds / pharmacology*
-
Bacteriophage T4
-
Benzamides / metabolism*
-
Benzamides / pharmacology*
-
Binding, Competitive
-
Cell Line, Tumor
-
Cell Proliferation / drug effects
-
DNA / metabolism*
-
DNA, Superhelical / metabolism
-
DNA, Viral / metabolism
-
Drug Design
-
Ethidium / metabolism
-
Humans
-
Inhibitory Concentration 50
-
Kinetics
-
Plasmids
-
Polydeoxyribonucleotides / metabolism
-
Serine Proteinase Inhibitors / metabolism*
-
Serine Proteinase Inhibitors / pharmacology*
-
Topoisomerase I Inhibitors / metabolism*
-
Topoisomerase I Inhibitors / pharmacology*
-
Topoisomerase II Inhibitors / metabolism*
-
Topoisomerase II Inhibitors / pharmacology*
Substances
-
Aniline Compounds
-
Benzamides
-
DNA, Superhelical
-
DNA, Viral
-
Polydeoxyribonucleotides
-
Serine Proteinase Inhibitors
-
Topoisomerase I Inhibitors
-
Topoisomerase II Inhibitors
-
DNA
-
calf thymus DNA
-
Ethidium