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

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...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1997/01/15, Vol.45(1), pp.134-137
Hauptverfasser:	HARADA, Naoyuki, KAWAGUCHI, Takayuki, INOUE, Isao, OHASHI, Motoaki, ODA, Kouji, HASHIYAMA, Tomiki, TSUJIHARA, Kenji
Format:	Artikel
Sprache:	eng
Schlagworte:	9-hydroxyellipticine 2-oxide Animals Antineoplastic agents Antineoplastic Agents - administration & dosage Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Biological and medical sciences Carcinoma, Lewis Lung - drug therapy colon 26 Colonic Neoplasms - drug therapy Drug Screening Assays, Antitumor Ellipticines - chemistry Ellipticines - pharmacology General aspects Leukemia P388 - drug therapy Lewis lung carcinoma Male Medical sciences Mice P388 leukemia Pharmacology. Drug treatments Rats water-soluble
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Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.45.134