Synthesis and Antitumor Activity of Novel Benzophenone Derivatives

Eiji KUMAZAWA; Kenji HIROTANI; S. Clifford BURFORD; Keiichi KAWAGOE; Tamotsu MIWA; Ikuo MITSUI; Akio EJIMA

doi:10.1248/cpb.45.1470

Eiji KUMAZAWA, Kenji HIROTANI, S. Clifford BURFORD, Keiichi KAWAGOE, Tamotsu MIWA, Ikuo MITSUI, Akio EJIMA

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Keywords: benzophenone, cytotoxic activity, antitumor activity

JOURNAL FREE ACCESS

1997 Volume 45 Issue 9 Pages 1470-1474

DOI https://doi.org/10.1248/cpb.45.1470

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Abstract

Novel benzophenone derivatives were synthesized and screened for cytotoxic and antitumor activity. Friedel-Crafts condensation was employed to construct the benzophenone skeleton. Among the compounds synthesized, morpholino and thiomorpholino benzophenones 3a-d exhibited potent cytotoxic activity against P388 murine leukemia and PC-6 human lung carcinoma cells in vitro, and compounds 3a, 3c, and 3j, when administered intraperitoneally, showed significant antitumor activity against the malignant ascites caused by intraperitoneal inoculation of P388 cells in mice.

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