8-苯基氨基嘧啶并[4,5-c]异喹啉醌的合成与抗肿瘤活性评价
Synthesis and antitumor evaluation of 8-phenylaminopyrimido[4,5-c]isoquinolinequinones.
作者信息
Vásquez David, Rodríguez Jaime A, Theoduloz Cristina, Verrax Julien, Calderon Pedro Buc, Valderrama Jaime A
机构信息
Facultad de Química, Pontificia Universidad Católica de Chile, Casilla 306, Santiago, Chile.
出版信息
Bioorg Med Chem Lett. 2009 Sep 1;19(17):5060-2. doi: 10.1016/j.bmcl.2009.07.041. Epub 2009 Jul 10.
A series of 8-phenylaminopyrimido[4,5-c]isoquinoline-7,10-quinone derivatives were prepared by regioselective amination reaction of pyrimido[4,5-c]isoquinoline-7,10-quinones with arylamines in the presence of a Lewis acid catalyst. Preliminary evaluation of the members of the series against cancer cell lines and assays of activation of their cytotoxic activity on K562 cells with ascorbic acid are reported.
通过嘧啶并[4,5-c]异喹啉-7,10-醌与芳胺在路易斯酸催化剂存在下的区域选择性胺化反应，制备了一系列8-苯基氨基嘧啶并[4,5-c]异喹啉-7,10-醌衍生物。报道了该系列成员对癌细胞系的初步评估以及它们在抗坏血酸存在下对K562细胞的细胞毒性活性激活测定。
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