Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC)

  • Bioorg Med Chem Lett. 2002 Oct 21;12(20):2919-23. doi: 10.1016/s0960-894x(02)00622-4.
Michael L Curtin  1 ,  Robert B Garland ,  H Robin Heyman ,  Robin R Frey ,  Michael R Michaelides ,  Junling Li ,  Lori J Pease ,  Keith B Glaser ,  Patrick A Marcotte ,  Steven K Davidsen
Affiliations
  • 1. Cancer Research Area, Abbott Laboratories, Dept. 47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA. [email protected]
PMID: 12270175 DOI: 10.1016/s0960-894x(02)00622-4
Abstract

A series of succinimide hydroxamic acids was prepared and evaluated in vitro for HDAC inhibition and tumor cell antiproliferation. While the original macrocyclic analogue 6 was quite potent in both assays, several appropriately substituted non-macrocyclic succinimides, such as 23, were equipotent.