346718-87-4Relevant academic research and scientific papers
5-LIPOXYGENASE INHIBITORS
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Page/Page column 34, (2009/12/28)
The use of compounds of the formula (I) Ar1-L1-Ar2-L2-C(R3)(R4)N(OR1)C(=Y)-R2 (I) where Y is selected from O or S; R1 is H, a salt or readily hydrolysable s
HDAC INHIBITORS
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Page/Page column 33, (2008/12/06)
The use of compounds of the formula (I): Ar1-L1-Ar2-L2-C(R3)(R4)N(OR1)C(=Y)-R2 where Y is selected from O or S; R1 is H, a salt or readily hydrolysable substituent; R2 is selected from H or CH3, CH2F, CF2H or CF3; R3 and R4 are selected independently from H, C1-4 alkyl or alkenyl, CF3, CH2F, CF2H and F, with the proviso that if either R3 or R4 is H, then the other is not H; L1 is a linker group; L2 is a linker group comprising an optionally substituted or unsubstituted unsaturated branched or straight chain alkyl group; Ar1 is an optionally substituted or unsubstituted aryl or heterocyclic group; and Ar2 is an optionally substituted or unsubstituted aryl or heterocyclic group, in the treatment of HDAC mediated diseases or diseases provide improved therapies due to the potent inhibition of HDAC and long duration of activity in vivo after oral administration. They are potential useful in diseases in which HDAC has been implicated, e.g. psoriasis, cancer, Alzheimer's disease, Huntington's disease and HIV.
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.
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.
