501682-96-8Relevant academic research and scientific papers
Carbamic acid compounds comprising a sulfonamide linkage as hdac inhibitors
-
, (2008/06/13)
This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S (═O)2NR1— and —NR1S(═O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(═O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
Polymer-assisted, multi-step solution phase synthesis and biological screening of histone deacetylase inhibitors
Bapna, Akanksha,Vickerstaffe, Emma,Warrington, Brian H.,Ladlow, Mark,Fan, Tai-Ping D.,Ley, Steven V.
, p. 611 - 620 (2007/10/03)
The polymer-assisted solution phase synthesis (PASP) of an array of histone deacetylase (HDAc) inhibitors is described. HDAc inhibitors have considerable potential as new anti-proliferative agents. Selected compounds were shown to inhibit both human endothelial cell proliferation, and the formation of tubules (neovascularisation) in an in vitro model of angiogenesis.
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.
