title: Synthesis, DNA binding, topoisomerases inhibition and cytotoxic properties of 4-arylcarboxamidopyrrolo-2-carboxyanilides.
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.
authors.affiliation: Institut de Chimie Pharmaceutique Albert Lespragnol, Université de Lille 2, France.
authors.forename: F
authors.initials: F
authors.lastname: Dudouit
authors.forename: J F
authors.initials: JF
authors.lastname: Goossens
authors.forename: R
authors.initials: R
authors.lastname: Houssin
authors.forename: J P
authors.initials: JP
authors.lastname: Hénichart
authors.forename: P
authors.initials: P
authors.lastname: Colson
authors.forename: C
authors.initials: C
authors.lastname: Houssier
authors.forename: N
authors.initials: N
authors.lastname: Gelus
authors.forename: C
authors.initials: C
authors.lastname: Bailly
mesh_terms: D000813:Anilides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D002942:Circular Dichroism; D004247:DNA / Q000378:metabolism*; D018983:DNA Footprinting; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D018922:HL-60 Cells; D006801:Humans; D011758:Pyrroles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D013696:Temperature; D059004:Topoisomerase I Inhibitors
chemical_list: D000813:Anilides; D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011758:Pyrroles; D059004:Topoisomerase I Inhibitors; D004247:DNA