pubmed:abstractText |
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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pubmed: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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