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CN105646495A 一种吡咯并[2,3-b]吡嗪衍生物及其制备方法和应用 无效 - 撤回

一种吡咯并[2,3-b]吡嗪衍生物及其制备方法和应用
摘要：
本发明提供了一种吡咯并[2,3-b]吡嗪衍生物，所述衍生物结构式如式（I）所示： 式I；其中，R1为氢、羟基、杂环基、苯基或取代苯基、胺基或取代胺基；R2为氰基、甲基或氢；n = 1、2、3、4、5、6、7或8；Y为NH、O、S或N(CH2)mR5，m=1、2、3、4、5或6；R5为氢、胺基或取代胺基。本发明提供的衍生物能够显著的抑制人DNA拓扑异构酶Ⅱ的活性及抑制DNA拓扑异构酶Ⅱ在肿瘤细胞株高表达，是抗肿瘤药物的重要靶标。同时，所述衍生物对多株肿瘤细胞增殖具有明显抑制作用，对白血病细胞具有明显诱导凋亡的能力，在制备抗肿瘤及抗白血病药物上具有广阔的应用空间。
摘要（英）：

The invention provides pyrrolo[2,3-b]pyrazine derivatives. The structural formula of the derivatives are disclosed as Formula (I), wherein R1 is hydrogen, hydroxyl, heterocyclic radical, phenyl or substituted phenyl, and amido or substituted amido; R2 is cyano, methyl or hydrogen; n=1, 2, 3, 4, 5, 6, 7 or 8; Y is NH, O, S or N(CH2)mR5; m=1, 2, 3, 4, 5 or 6; and R5 is hydrogen, amido or substituted amido. The derivatives provided by the invention can obviously inhibit activity of DNA topoismerase II and inhibit high expression of the DNA topoismerase II in tumor cell strains, and is an important target for antineoplastic drugs. Meanwhile, the derivatives have obvious inhibiting actions on proliferation of multiple tumor cell strains, have obvious capacity for inducing apoptosis of leukaemia cells, and have wide application prospects in preparing antitumor and anti-leukaemia drugs.

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