Analogues of antifungal tjipanazoles from rebeccamycin.
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.
Voldoire
Aline
A
Université Blaise Pascal, Synthèse et Etude de Systèmes à Intérêt Biologique, UMR 6504, 63177 Aubière, France.
Moreau
Pascale
P
Sancelme
Martine
M
Matulova
Maria
M
Léonce
Stéphane
S
Pierré
Alain
A
Hickman
John
J
Pfeiffer
Bruno
B
Renard
Pierre
P
Dias
Nathalie
N
Bailly
Christian
C
Prudhomme
Michelle
M
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
D000935:Antifungal Agents; D002227:Carbazoles; D006131:Growth Inhibitors; D007211:Indoles; C096121:tjipanazole D; C053339:rebeccamycin