Title of article :
Synthesis, DNA binding, topoisomerases inhibition and cytotoxic properties of 4-arylcarboxamidopyrrolo-2-carboxyanilides
Author/Authors :
Fabienne Dudouit، نويسنده , , Jean-François Goossens، نويسنده , , Raymond Houssin، نويسنده , , Jean-Pierre Hénichart، نويسنده , , Pierre Colson، نويسنده , , Claude Houssier، نويسنده , , Nathalie Gelus، نويسنده , , Christian Bailly، نويسنده ,
Abstract :
Three 4-arylcarboxamidopyrrolo-2-carboxyanilides bearing different substituents on the pyrrole nitrogen were synthesized and evaluated for their capacities to bind to specific sequences within the minor groove of DNA and to inhibit human topoisomerases I and II in vitro. The cytotoxicity of the drugs correlates with their DNA binding affinities. The two drugs bearing a N-methyl or N-benzyl pyrrole stabilize topoisomerase I-DNA complexes.
