Design and synthesis of novel class of CK2 inhibitors : application of copper- and gold-catalysed cascade reactions for fused nitrogen heterocycles.
Design and synthesis of novel class of CK2 inhibitors : application of copper- and gold-catalysed cascade reactions for fused nitrogen heterocycles.
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新型 CK2 抑制剂的设计和合成：铜和金催化的稠合氮杂环级联反应的应用。
DOI：
10.1039/c2ob25298h
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发表时间：
2012
期刊：
影响因子：
--
通讯作者：
Fujii N.
中科院分区：
文献类型：
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作者：
Suzuki Y;Oishi S;Takei Y;Yasue M;Misu R;Naoe S;Hou Z;Kure T;Nakanishi I;Ohno H;Hirasawa A;Tsujimoto G;Fujii N.
在前人构效关系（SAR）研究的基础上，设计了两类融合氮杂环作为CK2抑制剂的候选化合物。利用过渡金属催化的级联反应和/或多组分反应制备了各种双吡咯[3,2-b:2 ',3 ' -e]吡啶和苯并[g]茚唑衍生物。这些候选药物的生物学评价表明，苯并[g]吲哚唑是一种很有前途的支架，可以作为有效的CK2抑制剂。这些有效的CK2抑制剂对细胞增殖的抑制活性也被提出。
Two classes of fused nitrogen heterocycles were designed as CK2 inhibitor candidates on the basis of previous structure–activity relationship (SAR) studies. Various dipyrrolo[3,2-b:2′,3′-e]pyridine and benzo[g]indazole derivatives were prepared using transition-metal-catalysed cascade and/or multicomponent reactions. Biological evaluation of these candidates revealed that benzo[g]indazole is a promising scaffold for potent CK2 inhibitors. The inhibitory activities on cell proliferation of these potent CK2 inhibitors are also presented.