723757-78-6Relevant articles and documents
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors
Bouchain, Giliane,Leit, Silvana,Frechette, Sylvie,Abou Khalil, Elie,Lavoie, Rico,Moradei, Oscar,Woo, Soon Hyung,Fournel, Marielle,Yan, Pu T.,Kalita, Ann,Trachy-Bourget, Marie-Claude,Beaulieu, Carole,Li, Zuomei,Robert, Marie-France,MacLeod, A. Robert,Besterman, Jeffrey M.,Delorme, Daniel
, p. 820 - 830 (2007/10/03)
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.
Design and synthesis of a novel class of histone deacetylase inhibitors.
Lavoie,Bouchain,Frechette,Woo,Abou-Khalil,Leit,Fournel,Yan,Trachy-Bourget,Beaulieu,Li,Besterman,Delorme
, p. 2847 - 2850 (2007/10/03)
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.
