Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
Org Biomol Chem. 2013 May 28;11(20):3288-96. doi: 10.1039/c3ob40223a.
Pyrazolo[4,3-b]indole derivatives have been designed as novel CK2 inhibitor compounds based on the binding mode analysis of a previously reported phenylpyrazole-type CK2 inhibitor. A series of pyrazolo[4,3-b]indoles and related dihydropyrazolo[4,3-b]indoles were efficiently prepared from simple starting materials using a gold-catalysed three-component annulation reaction as a key step. Several of the newly synthesized compounds displayed high levels of inhibitory activity, indicating that the pyrazolo[4,3-b]indole core represents a promising scaffold for the development of potent CK2 inhibitors.
吡唑并[4,3-b]吲哚衍生物被设计为新型 CK2 抑制剂化合物，基于先前报道的苯并吡唑型 CK2 抑制剂的结合模式分析。使用金催化的三组分环化反应作为关键步骤，从简单的起始原料高效制备了一系列吡唑并[4,3-b]吲哚和相关的二氢吡唑并[4,3-b]吲哚。新合成的几种化合物表现出高抑制活性，表明吡唑并[4,3-b]吲哚核心代表了开发有效 CK2 抑制剂的有前途的支架。
