Design and synthesis of a novel class of histone deacetylase inhibitors

  • Bioorg Med Chem Lett. 2001 Nov 5;11(21):2847-50. doi: 10.1016/s0960-894x(01)00552-2.
R Lavoie  1 ,  G Bouchain ,  S Frechette ,  S H Woo ,  E Abou-Khalil ,  S Leit ,  M Fournel ,  P T Yan ,  M C Trachy-Bourget ,  C Beaulieu ,  Z Li ,  J Besterman ,  D Delorme
Affiliations
  • 1. Department of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montréal, Québec, Canada H4S 2A1.
PMID: 11597413 DOI: 10.1016/s0960-894x(01)00552-2
Abstract

Histone deacetylase inhibitors (HDACs) have emerged as a novel class of antiproliferative agents. Utilizing structure-based design, the synthesis of a series of sulfonamide hydroxamic acids is described. Further optimization of this series by substitution of the terminal aromatic ring yielded HDAC inhibitors with good in vitro and in vivo activities.