1. Academic Validation
  2. Succinimide hydroxamic acids as potent inhibitors of histone deacetylase (HDAC)

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

Affiliation

  • 1 Cancer Research Area, Abbott Laboratories, Dept. 47J, Bldg. AP10, 100 Abbott Park Road, Abbott Park, IL 60064, USA. mike.curtin@abbott.com
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.

Figures