2. Academic Validation
  3. Sulfamides as novel histone deacetylase inhibitors

Sulfamides as novel histone deacetylase inhibitors

  • Bioorg Med Chem Lett. 2009 Jan 15;19(2):336-40. doi: 10.1016/j.bmcl.2008.11.081.
Amal Wahhab 1,  David Smil,  Alain Ajamian,  Martin Allan,  Yves Chantigny,  Eric Therrien,  Natalie Nguyen,  Sukhdev Manku,  Silvana Leit,  Jubrail Rahil,  Andrea J Petschner,  Ai-Hua Lu,  Alina Nicolescu,  Sylvain Lefebvre,  Samuel Montcalm,  Marielle Fournel,  Theresa P Yan,  Zuomei Li,  Jeffrey M Besterman,  Robert Déziel
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, MethylGene Inc., 7220 rue Frederick-Banting, Montreal, Que., Canada H4S 2A1. wahhaba@methylgene.com
PMID: 19084395 DOI: 10.1016/j.bmcl.2008.11.081
Abstract

The sulfamide moiety has been utilized to design novel HDAC inhibitors. The potency and selectivity of these inhibitors were influenced both by the nature of the scaffold, and the capping group. Linear long-chain-based analogs were primarily HDAC6-selective, while analogs based on the lysine scaffold resulted in potent HDAC1 and HDAC6 inhibitors.

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