Indole amide hydroxamic acids as potent inhibitors of histone deacetylases |
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Authors: | Dai Yujia Guo Yan Guo Jun Pease Lori J Li Junling Marcotte Patrick A Glaser Keith B Tapang Paul Albert Daniel H Richardson Paul L Davidsen Steven K Michaelides Michael R |
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Affiliation: | Cancer Research, Abbott Laboratories, Dept. R47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064-6100, USA. yujia.dai@abbott.com |
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Abstract: | 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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