| Literature DB >> 18182289 |
Joey L Methot1, 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, Candia M Kenific, Astrid M Kral, Peter T Meinke, Richard E Middleton, Nicole Ozerova, David L Sloman, Matthew G Stanton, Alexander A Szewczak, Sriram Tyagarajan, David J Witter, J Paul Secrist, Thomas A Miller.
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.Entities:
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Year: 2008 PMID： 18182289 DOI： 10.1016/j.bmcl.2007.12.031
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823