抗肿瘤咪唑并吖啶酮类化合物的构效关系：体内合成及抗白血病活性
Structure-activity relationship for antineoplastic imidazoacridinones: synthesis and antileukemic activity in vivo.
作者信息
Cholody W M, Horowska B, Paradziej-Lukowicz J, Martelli S, Konopa J
机构信息
Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdansk, Gdansk, Poland.
出版信息
J Med Chem. 1996 Mar 1;39(5):1028-32. doi: 10.1021/jm950564r.
Synthesis of several new 5-amino-substituted derivatives of 5-amino-6H-imidazo[4,5,1-de]-acridin-6-one bearing in the benzene ring OH, OCH3, CH3, tert-butyl, or OCH2O groups is described. 8-OH-substituted compounds or double-substituted 7-OH-10-OCH3 compounds demonstrated potent in vivo activity against murine P388 leukemia. The highest activity was exhibited by 5-[[2-[[2-(diethylamino)ethyl]amino]ethyl]amino]-8-hydroxy-6H- imidazo[4,5,1-de]-acridin-6-one (4c).
描述了几种新的5-氨基-6H-咪唑并[4,5,1-de] -吖啶-6-酮的5-氨基取代衍生物的合成，这些衍生物在苯环上带有OH、OCH3、CH3、叔丁基或OCH2O基团。8-OH取代的化合物或双取代的7-OH-10-OCH3化合物对小鼠P388白血病显示出有效的体内活性。5-[[2-[[2-(二乙氨基)乙基]氨基]乙基]氨基]-8-羟基-6H-咪唑并[4,5,1-de] -吖啶-6-酮(4c)表现出最高活性。
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