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.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Andreani A,Granaiola M,Leoni A,Locatelli A,Morigi R,Rambaldi M,Varoli L,Lannigan D,Smith J,Scudiero D,Kondapaka S,Shoemaker RHdoi
10.1016/j.ejmech.2011.07.001subject
Has Abstractpub_date
2011-09-01 00:00:00pages
4311-23issue
9eissn
0223-5234issn
1768-3254pii
S0223-5234(11)00514-9journal_volume
46pub_type
杂志文章abstract：:In this study, a collection of N-(6-mercaptohexyl)-3-substituted-1H-pyrazole-5-carboxamide HDAC inhibitors was developed. Among them, 15k was identified as the most potent inhibitor against total HDACs with IC50 of 0.008 μM. Further isoenzyme assays revealed that 15k and its analogs have a preference for HDAC1-3 (clas...
journal_title：European journal of medicinal chemistry
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journal_title：European journal of medicinal chemistry
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journal_title：European journal of medicinal chemistry
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