Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors.

Abstract

A lead benzamide, 3, was identified as a potent and low molecular weight histone deacetylase (HDAC) inhibitor. Optimization led to 16d, demonstrating an excellent balance of efficacy and non-efficacy properties, along with very desirable in vivo DMPK. The final compounds presented are >1000-fold more potent than the initial screen hit, an improvement in… (More)
DOI: 10.1016/j.bmcl.2008.03.041

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@article{Andrews2008DesignAC, title={Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors.}, author={David Andrews and Elaine S. E. Stokes and Greg R Carr and Zbigniew S Matusiak and Craig A. Roberts and Michael J. Waring and Madeleine C. Brady and Christine M. Chresta and Simon J East}, journal={Bioorganic & medicinal chemistry letters}, year={2008}, volume={18 8}, pages={2580-4} }