2. Academic Validation
  3. Indole amide hydroxamic acids as potent inhibitors of histone deacetylases

Indole amide hydroxamic acids as potent inhibitors of histone deacetylases

  • Bioorg Med Chem Lett. 2003 Jun 2;13(11):1897-901. doi: 10.1016/s0960-894x(03)00301-9.
Yujia Dai 1,  Yan Guo,  Jun Guo,  Lori J Pease,  Junling Li,  Patrick A Marcotte,  Keith B Glaser,  Paul Tapang,  Daniel H Albert,  Paul L Richardson,  Steven K Davidsen,  Michael R Michaelides
Affiliations

Affiliation

  • 1 Cancer Research, Abbott Laboratories, Dept. R47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064-6100, USA. [email protected]
PMID: 12749893 DOI: 10.1016/s0960-894x(03)00301-9
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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