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
✍ Scribed by Robert K. Y. Zee-Cheng; C. C. Cheng
- Publisher
- John Wiley and Sons
- Year
- 1982
- Tongue
- English
- Weight
- 188 KB
- Volume
- 71
- Category
- Article
- ISSN
- 0022-3549
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✦ Synopsis
An oxygen analog of the antineoplastic anthraquinone, 1,4-dihydroxy-5,8-bis[ [2-(2-hydroxyethyl)amino]ethyl)amino -9,lO -anthracenedione, was synthesized. This compound, 1,4-dihydroxy-5,8bis[ [2-(2-hydroxyethoxy)ethyI]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-0-0 triangulation hypothesis was discussed. Keyphrases Antineoplastic agents-structure-activity relationship, 5,8-bis[[2-(2-hydroxyethoxy)ethyl]amino]-9,l0-anthracenedione 0 Structure-activity relationships-5, 8-bis[ [2-(2-hydroxyethoxy)ethyl]amino]-9,10-anthracenedione Anthraquinones-antineoplastic agents, 5,8-bis[[2-(2-hydroxyethoxy)ethyl]amino)g,lO-anthracenedione, structure-activity relationships The importance of the nitrogen atom in the center of the side chain of 1,4-dihydroxy-5,8-bis[ [2-(2-hydroxyethyl)-For the general screening procedure. see Ref. 1'1. For the test data interpretation. see Instruction Booklet 14, "Screening Data Summary Interpretation and Outlinr of'Current Screen," Dru Evaluation Branch, Divisinn of Cancer Treatment, National Cancer Institute, tethesda, MD 20014. Ln general. a minimum increare in survival ( i f treated animals over controls result ing in a 'r/C 2 1 3 " k is iiecesmry lor a compnund to be considered as active.