1.
Bioorg Med Chem Lett
; 10(6): 553-7, 2000 Mar 20.
Artigo
em Inglês
| MEDLINE
| ID: mdl-10741552
RESUMO
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.