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

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Andreani A, Granaiola M, Leoni A, Locatelli A, Morigi R, Rambaldi M, Varoli L, Lannigan D, Smith J, Scudiero D, Kondapaka S, Shoemaker RH

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.

PubMed ID

21794960 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Staurosporine	Tyrosine-protein kinase Lck	IC 50 (nM)	1.33	N/A	N/A	Details
Staurosporine	Tyrosine-protein kinase ZAP-70	IC 50 (nM)	8.63	N/A	N/A	Details