Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377326 | Bioorganic & Medicinal Chemistry Letters | 2008 | 6 Pages |
Abstract
We report herein the initial exploration of novel selective HDAC1/HDAC2 inhibitors (SHI-1:2). Optimized SHI-1:2 structures exhibit enhanced intrinsic activity against HDAC1 and HDAC2, and are greater than 100-fold selective versus other HDACs, including HDAC3. Based on the SAR of these agents and our current understanding of the HDAC active site, we postulate that the SHI-1:2 extend the existing HDAC inhibitor pharmacophore to include an internal binding domain.
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Related Topics
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Organic Chemistry
Authors
Joey L. Methot, Prasun K. Chakravarty, Melissa Chenard, Joshua Close, Jonathan C. Cruz, William K. Dahlberg, Judith Fleming, Christopher L. Hamblett, Julie E. Hamill, Paul Harrington, Andreas Harsch, Richard Heidebrecht, Bethany Hughes, Joon Jung,