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 inhibitors.

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Abstract

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.

Journal

  • Organic & biomolecular chemistry

    Organic & biomolecular chemistry 11(20), 3288-3296, 2013-05-28

    Royal Society of Chemistry

Codes

  • NII Article ID (NAID)
    120005474525
  • Text Lang
    ENG
  • Article Type
    journal article
  • ISSN
    1477-0539
  • Data Source
    IR 
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