2. Academic Validation
  3. Design and synthesis of a novel class of histone deacetylase inhibitors

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

Affiliation

  • 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.

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