1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases

Raj N. Misra, David B. Rawlins, Hai Yun Xiao, Weifang Shan, Isia Bursuker, Kristin A. Kellar, Janet G. Mulheron, John S. Sack, John S. Tokarski, S. David Kimball, Kevin R. Webster

Research output: Contribution to journalArticle

60 Scopus citations

Abstract

1H-Pyrazolo[3,4-b]pyridine 3 (SQ-67563) has been shown to be a potent, selective inhibitor of CDK1/CDK2 in vitro. In cells 3 acts as a cytotoxic agent with the ability to block cell cycle progression and/or induce apoptosis. The solid state structure of 3 bound to CDK2 shows 3 resides coincident with the ATP purine binding site and forms important H-bonding interactions with Leu83 on the protein backbone.

Original languageEnglish (US)
Pages (from-to)1133-1136
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume13
Issue number6
DOIs
StatePublished - Mar 24 2003
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Molecular Medicine
  • Molecular Biology
  • Biochemistry
  • Clinical Biochemistry
  • Pharmaceutical Science
  • Organic Chemistry

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  • Cite this

    Misra, R. N., Rawlins, D. B., Xiao, H. Y., Shan, W., Bursuker, I., Kellar, K. A., Mulheron, J. G., Sack, J. S., Tokarski, J. S., Kimball, S. D., & Webster, K. R. (2003). 1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases. Bioorganic and Medicinal Chemistry Letters, 13(6), 1133-1136. https://doi.org/10.1016/S0960-894X(03)00034-9