Synthesis and Antitumor Activity of Quaternary Salts of 2-(2'-Oxoalkoxy)-9-hydroxyellipticines

Naoyuki HARADA; Takayuki KAWAGUCHI; Isao INOUE; Motoaki OHASHI; Kouji ODA; Tomiki HASHIYAMA; Kenji TSUJIHARA

doi:10.1248/cpb.45.134

Naoyuki HARADA, Takayuki KAWAGUCHI, Isao INOUE, Motoaki OHASHI, Kouji ODA, Tomiki HASHIYAMA, Kenji TSUJIHARA

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Keywords: 9-hydroxyellipticine 2-oxide, water-soluble, P388 leukemia, colon 26, Lewis lung carcinoma

JOURNAL FREE ACCESS

1997 Volume 45 Issue 1 Pages 134-137

DOI https://doi.org/10.1248/cpb.45.134

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Abstract

Various kinds of water-soluble quaternary salts of 2-(2'-oxoalkoxy)-9-hydroxyellipticines were synthesized in a search for compounds with potent antitumor activity and low toxicity. Some compounds exhibited more potent antitumor activities than elliptinium (1) and SUN 4599 (3). In particular, 2-(3'-methoxy-2'-oxopropanoxy)-9-hydroxy-5, 11-dimethyl-6H-pyrido[4, 3-b]carbazolium bromide (4d) showed potent antitumor activities against P388 leukemia, colon 26, and Lewis lung carcinoma.

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