2. Academic Validation
  3. Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors

Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors

  • J Med Chem. 2003 Feb 27;46(5):820-30. doi: 10.1021/jm020377a.
Giliane Bouchain 1,  Silvana Leit,  Sylvie Frechette,  Elie Abou Khalil,  Rico Lavoie,  Oscar Moradei,  Soon Hyung Woo,  Marielle Fournel,  Pu T Yan,  Ann Kalita,  Marie-Claude Trachy-Bourget,  Carole Beaulieu,  Zuomei Li,  Marie-France Robert,  A Robert MacLeod,  Jeffrey M Besterman,  Daniel Delorme
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, MethylGene Inc., 7220 Frederick-Banting, Montréal, Québec H4S 2A1, Canada.
PMID: 12593661 DOI: 10.1021/jm020377a
Abstract

A series of sulfonamide hydroxamic acids and anilides have been synthesized and studied as histone deacetylase (HDAC) inhibitors that can induce hyperacetylation of histones in human Cancer cells. The inhibition of HDAC activity represents a novel approach for intervening in cell cycle regulation. The lead candidates were screened in a panel of human tumor and normal cell lines. They selectively inhibit proliferation, cause cell cycle blocks, and induce Apoptosis in human Cancer cells but not in normal cells. The structure-activity relationships, the antiproliferative activity, and the in vivo efficacy are described.

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