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Development of Potential Antitumor Agents. Synthesis and Biological Evaluation of a New Set of Sulfonamide Derivatives as Histone Deacetylase Inhibitors

2003; American Chemical Society; Volume: 46; Issue: 5 Linguagem: Inglês

10.1021/jm020377a

1520-4804

Giliane Bouchain, Silvana Leit, Sylvie Fréchette, Elie Abou Khalil, Rico Lavoie, Oscar Moradei, Soon Hyung Woo, Marielle Fournel, Pu Yan, Ann Kalita, Marie-Claude Trachy-Bourget, Carole Beaulieu, Zuomei Li, Marie‐France Robert, A. Robert MacLeod, Jeffrey M. Besterman, Daniel Delorme,

Protein Degradation and Inhibitors

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.