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1,4-双（氨基链烷酰胺基）-9,10-蒽二酮的合成与抗肿瘤活性评价

Synthesis and antineoplastic evaluation of 1,4-bis(aminoalkanamido)-9,10-anthracenediones.

作者信息

Martelli S, Dzieduszycka M, Stefanska B, Bontemps-Gracz M, Borowski E

机构信息

Department of Chemical Sciences, University of Camerino, Italy.

出版信息

J Med Chem. 1988 Oct;31(10):1956-9. doi: 10.1021/jm00118a015.

DOI:10.1021/jm00118a015
PMID:3172129
Abstract

The effect of the replacement of amino groups, attached to the anthraquinone ring in [(aminoalkyl)amino]-anthraquinones, by an amido function on DNA binding, cytotoxicity, and antileukemic activity has been studied. The corresponding 1,4-bis(aminoalkanamido)-9,10-anthracenediones have been synthesized and examined. It has been concluded that such modification does not exclude the DNA binding and cytotoxicity of mentioned compounds but decreases or abolishes the in vivo antileukemic activity.

摘要

研究了在[(氨基烷基)氨基]-蒽醌中连接在蒽醌环上的氨基被酰胺官能团取代对DNA结合、细胞毒性和抗白血病活性的影响。已合成并检测了相应的1,4-双(氨基烷酰胺基)-9,10-蒽二酮。得出的结论是，这种修饰并不排除上述化合物的DNA结合和细胞毒性，但会降低或消除其体内抗白血病活性。

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