Diversity-oriented synthesis of pyrazolo[4,3-b]indoles by gold-catalysed three-component annulation: application to the development of a new class of CK2 inhibitorsElectronic supplementary information (ESI) available. See DOI: 10.1039/c3ob40223a

• Main Authors: Hou, Zengye, Oishi, Shinya, Suzuki, Yamato, Kure, Tatsuhide, Nakanishi, Isao, Hirasawa, Akira, Tsujimoto, Gozoh, Ohno, Hiroaki, Fujii, Nobutaka
• Format: Article
• Language: English
• ISSN: 1477-0520; 1477-0539
• 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. Diversity-oriented synthesis of pyrazolo[4,3-b]indoles was developed using a gold-catalysed three-component annulation for the development of novel CK2 inhibitors.