Imidazo[2,1-b]thiazole guanylhydrazones as RSK2 inhibitors

Eur J Med Chem. 2011 Sep;46(9):4311-23. doi: 10.1016/j.ejmech.2011.07.001. Epub 2011 Jul 8.


The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most active compounds indicates a high degree of selectivity for inhibition of RSK2 compared to a spectrum of other related kinases. Selective inhibition of the MCF-7 breast tumor cell line compared to MCF-10A non-transformed cells, as well as selective inhibition of the biomarker GSK3 provides evidence that the compounds can affect the RSK2 target in cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Drug Screening Assays, Antitumor
  • Enzyme Inhibitors / pharmacology*
  • Glycogen Synthase Kinase 3 / antagonists & inhibitors
  • Humans
  • Hydrazones / pharmacology*
  • Magnetic Resonance Spectroscopy
  • Ribosomal Protein S6 Kinases / antagonists & inhibitors*
  • Spectrophotometry, Infrared


  • Enzyme Inhibitors
  • Hydrazones
  • Ribosomal Protein S6 Kinases
  • Glycogen Synthase Kinase 3