Design and synthesis of a novel class of CK2 inhibitors: application of copper- and gold-catalysed cascade reactions for fused nitrogen heterocycles

作者：Suzuki Yamato; Oishi Shinya^*; Takei Yoshinori; Yasue Misato; Misu Ryosuke; Naoe Saori; Hou Zengye; Kure Tatsuhide; Nakanishi Isao; Ohno Hiroaki; Hirasawa Akira; Tsujimoto Gozoh; Fujii Nobutaka

来源：Organic and Biomolecular Chemistry, 2012, 10(25): 4907-4915.

DOI：10.1039/c2ob25298h

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.

• 出版日期2012