Bioorg Med Chem Lett
Merck Research Laboratories, MSD, PO Box 20, 5340 BH Oss, The Netherlands.
Published: January 2012
Optimization of our previously described pyrrolopiperidone series led to the identification of a new benzamide sub-series, which exhibits consistently high potency in biochemical and cell-based assays throughout the series. Strong inhibition of LPS-induced production of the cytokine TNFα is coupled to the regulation of HSP27 phosphorylation, indicating that the observed cellular effects result from the inhibition of MK2. X-ray crystallographic and computational analyses provide a rationale for the high potency of the series.
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http://dx.doi.org/10.1016/j.bmcl.2011.10.071 | DOI Listing |
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