Synthesis and Antitumor Activity of 9-Acyloxyellipticines

Naoyuki HARADA; Kunihiko OZAKI; Kouji ODA; Noriyuki NAKANISHI; Motoaki OHASHI; Tomiki HASHIYAMA; Kenji TSUJIHARA

doi:10.1248/cpb.45.1156

Naoyuki HARADA, Kunihiko OZAKI, Kouji ODA, Noriyuki NAKANISHI, Motoaki OHASHI, Tomiki HASHIYAMA, Kenji TSUJIHARA

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Keywords: 9-acyloxyellipticine, water-soluble antitumor substance, P388 leukemia, Lewis lung carcinoma, B16 melanoma

JOURNAL FREE ACCESS

1997 Volume 45 Issue 7 Pages 1156-1162

DOI https://doi.org/10.1248/cpb.45.1156

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Abstract

Various kinds of water-soluble 9-acyloxyellipticine derivatives were synthesized in a search for compounds with potent antitumor activity. Antitumor activities against several tumors in mice (P388 leukemia, colon 26, Lewis lung carcinoma and B16 melanoma) were evaluated by using intravenous administration. Many compounds exhibited good antitumor activities; in particular, the glutarate derivative (5o) showed potent antitumor activity. This comopound (5o) may be converted to 9-hydroxyellipticine (2) by enzyme-catalyzed hydrolysis in the body.

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