Title of article
Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1)
Author/Authors
Kevin J. Wilson، نويسنده , , David J. Witter، نويسنده , , Jonathan B. Grimm، نويسنده , , Phieng Siliphaivanh، نويسنده , , Karin M. Otte، نويسنده , , Astrid M. Kral، نويسنده , , Judith C. Fleming، نويسنده , , Andreas Harsch، نويسنده , , Julie E. Hamill، نويسنده , , Jonathan C. Cruz، نويسنده , , Melissa Chenard، نويسنده , , Alexander A. Szewczak، نويسنده , , Richard E. Middleton، نويسنده , , Bethany L. Hughes، نويسنده , , William K. Dahlberg، نويسنده , , J. Paul Secrist، نويسنده , , Thomas A. Miller، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
1859
To page
1863
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.
Keywords
Selective , Benzamide , biaryl , HDAC1 inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799261
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