title: Analogues of antifungal tjipanazoles from rebeccamycin.
abstract: Analogues of antifungal tjipanazoles were obtained by semi-synthesis from rebeccamycin, an antitumor antibiotic isolated from cultures of Saccharothrix aerocolonigenes. The antiproliferative activities of the new compounds were evaluated in vitro against nine tumor cell lines. The effect on the cell cycle of murine leukemia L1210 cells was examined and the antimicrobial activities against two Gram positive bacteria, a Gram negative bacterium and a yeast were determined. The inhibitory properties toward four kinases and toward topoisomerase I were evaluated. The most cytotoxic compound in the series was a dinitro derivative characterized as a potent topoisomerase I inhibitor.
authors.affiliation: Université Blaise Pascal, Synthèse et Etude de Systèmes à Intérêt Biologique, UMR 6504, 63177 Aubière, France.
authors.forename: Aline
authors.initials: A
authors.lastname: Voldoire
authors.forename: Pascale
authors.initials: P
authors.lastname: Moreau
authors.forename: Martine
authors.initials: M
authors.lastname: Sancelme
authors.forename: Maria
authors.initials: M
authors.lastname: Matulova
authors.forename: Stéphane
authors.initials: S
authors.lastname: Léonce
authors.forename: Alain
authors.initials: A
authors.lastname: Pierré
authors.forename: John
authors.initials: J
authors.lastname: Hickman
authors.forename: Bruno
authors.initials: B
authors.lastname: Pfeiffer
authors.forename: Pierre
authors.initials: P
authors.lastname: Renard
authors.forename: Nathalie
authors.initials: N
authors.lastname: Dias
authors.forename: Christian
authors.initials: C
authors.lastname: Bailly
authors.forename: Michelle
authors.initials: M
authors.lastname: Prudhomme
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D002227:Carbazoles / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D045744:Cell Line, Tumor; D006131:Growth Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D051379:Mice
chemical_list: D000935:Antifungal Agents; D002227:Carbazoles; D006131:Growth Inhibitors; D007211:Indoles; C096121:tjipanazole D; C053339:rebeccamycin