Synthesis and Biological Evaluation of 6-(9-Hydroxy-5-methyl (and 5, 6-Dimethyl)-6H-pyrido[4, 3-b]carbazol-1-yl)picolinic Amides as New Olivacine Derivatives

Starting from 2-(6-methoxy-1-methylcarbazol-2-yl)ethylamine and diethyl-2, 6-pyridine dicarboxylate, the title compounds were obtained through five or six steps. The new compounds retained significant cytotoxicity towards various tumor cell lines, but in vivo studies on murine P388 leukemia, B16 mel...

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Veröffentlicht in:Chemical & pharmaceutical bulletin 1996/11/15, Vol.44(11), pp.2169-2172
Hauptverfasser: LANDRAS, Corinne, JASZTOLD-HOWORKO, Richard, PIERRE, Alain, LEONCE, Stephane, GUILBAUD, Nicolas, KRAUS-BERTHIER, Laurence, GUILLONNEAU, Claude, ROLLAND, Yves, ATASSI, Ghanem, BISAGNI, Emile
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Sprache:eng
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Zusammenfassung:Starting from 2-(6-methoxy-1-methylcarbazol-2-yl)ethylamine and diethyl-2, 6-pyridine dicarboxylate, the title compounds were obtained through five or six steps. The new compounds retained significant cytotoxicity towards various tumor cell lines, but in vivo studies on murine P388 leukemia, B16 melanoma and Lewis lung carcinoma showed a lowered antitumor activity with respect to that of the related ovivacine lead compound 1.
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.44.2169