title: Indolizino[1,2-b]quinolines derived from A-D rings of camptothecin: synthesis and DNA interaction.
abstract: Camptothecin consists of a lactone E-ring adjacent to a tetracyclic A-D ring planar chromophore which are essential for topoisomerase I inhibition and DNA interaction, respectively. The A-D ring system can be exploited to develop DNA-binding molecules. Indolizino[1,2-b]quinoline derivatives substituted with a piperidinoethyloxy side chain on the A-ring and an aminomethyl function on the D one were synthesized and their DNA-binding properties and in vitro cytotoxicity investigated.
authors.affiliation: Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, BP 83, 59006 Lille, France.
authors.forename: Aurore
authors.initials: A
authors.lastname: Perzyna
authors.forename: Raymond
authors.initials: R
authors.lastname: Houssin
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Goossens
authors.forename: Nicole
authors.initials: N
authors.lastname: Pommery
authors.forename: Carine
authors.initials: C
authors.lastname: Marty
authors.forename: Michael
authors.initials: M
authors.lastname: Facompré
authors.forename: Pierre
authors.initials: P
authors.lastname: Colson
authors.forename: Claude
authors.initials: C
authors.lastname: Houssier
authors.forename: Christian
authors.initials: C
authors.lastname: Bailly
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Hénichart
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002166:Camptothecin / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D004247:DNA / Q000737:chemistry* / Q000378:metabolism; D018983:DNA Footprinting; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D011471:Prostatic Neoplasms / Q000473:pathology; D013329:Structure-Activity Relationship; D013950:Thymus Gland / Q000378:metabolism; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D004247:DNA; D002166:Camptothecin