| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374460 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
The successful application of both solid and solution phase library synthesis, combined with tight integration into the medicinal chemistry effort, resulted in the efficient optimization of a novel structural series of selective HDAC1/HDAC2 inhibitors by the MRL-Boston Parallel Medicinal Chemistry group. An initial lead from a small parallel library was found to be potent and selective in biochemical assays. Advanced compounds were the culmination of iterative library design and possess excellent biochemical and cellular potency, as well as acceptable PK and efficacy in animal models.
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Related Topics
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Authors
Solomon D. Kattar, Laura M. Surdi, Anna Zabierek, Joey L. Methot, Richard E. Middleton, Bethany Hughes, Alexander A. Szewczak, William K. Dahlberg, Astrid M. Kral, Nicole Ozerova, Judith C. Fleming, Hongmei Wang, Paul Secrist, Andreas Harsch,