Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.


A series of hydroxamic acid-based HDAC inhibitors with an indole amide residue at the terminus have been synthesized and evaluated. Compounds with a 2-indole amide moiety have been found as the most active inhibitors among the different regioisomers. Introduction of substituents on the indole ring further improved the potency and generated a series of very potent inhibitors with significant antiproliferative activity. A representative compound in the series, 7b, has been found to be orally active in tumor growth inhibition model.


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@article{Dai2003IndoleAH, title={Indole amide hydroxamic acids as potent inhibitors of histone deacetylases.}, author={Yujia Dai and Yan Guo and Jun Guo and Lori J Pease and Junling Li and Patrick A Marcotte and Keith B. Glaser and Paul H Tapang and Daniel H. Albert and Paul L. Richardson and Steven K. Davidsen and Michael Michaelides}, journal={Bioorganic & medicinal chemistry letters}, year={2003}, volume={13 11}, pages={1897-901} }