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An oxygen analog of the antineoplastic anthraquinone, 1,4-dihydroxy-5,8-bis[[2-(2-hydroxyethyl)amino]ethyl]amino - 9,10-anthracenedione, was synthesized. This compound, 1,4-dihydroxy-5,8-bis[[2-(2-hydroxyethoxy)ethyl]amino] - 9,10-anthracenedione, was found to be inactive against P-388 lymphocytic leukemia. A comparative structure-activity study of these two anthraquinones in terms of previously postulated N--O--O triangulation hypothesis was discussed.


R K Zee-Cheng, C C Cheng. Structure-activity relationship study of anthraquinones: 1,4-dihydroxy-5,8-bis[[2-(2-hydroxyethoxy)ethyl]amino]-9,10-anthracenedione, an analog of an established antineoplastic agent. Journal of pharmaceutical sciences. 1982 Jun;71(6):708-9

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PMID: 7097541

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