Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).

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Bioorganic & Medicinal Chemistry Letters. 2008 Mar 15;18(6):1859-63. doi: 10.1016/j.bmcl.2008.02.012
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Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).
Wilson KJ, Witter DJ, Grimm JB, Siliphaivanh P, Otte KM, Kral AM, Fleming JC, Harsch A, Hamill JE, Cruz JC, Chenard M, Szewczak AA, Middleton RE, Hughes BL, Dahlberg WK, Secrist JP, Miller TA
Note: Research in this publication was not performed at Janelia.
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Abstract

An HTS screening campaign identified a series of low molecular weight phenols that showed excellent selectivity (>100-fold) for HDAC1/HDAC2 over other Class I and Class II HDACs. Evolution and optimization of this HTS hit series provided HDAC1-selective (SHI-1) compounds with excellent anti-proliferative activity and improved physical properties. Dose-dependent efficacy in a mouse HCT116 xenograft model was demonstrated with a phenylglycine SHI-1 analog.

PMID: 18304810 [PubMed - indexed for MEDLINE]

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Janelia Authors

Jonathan Grimm
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