623588-14-7Relevant academic research and scientific papers
Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors
Hiranaka, Seiya,Tega, Yuma,Higuchi, Kei,Kurosawa, Toshiki,Deguchi, Yoshiharu,Arata, Mayumi,Ito, Akihiro,Yoshida, Minoru,Nagaoka, Yasuo,Sumiyoshi, Takaaki
supporting information, p. 884 - 888 (2018/09/12)
We designed and synthesized a pyrilamine derivative 1 as a selective class I HDAC inhibitor that targets pyrilamine-sensitive proton-coupled organic cation antiporter (PYSOCA) at the blood-brain barrier (BBB). Introduction of pyrilamine moiety to benzamid
Delayed and prolonged histone hyperacetylation with a selective HDAC1/HDAC2 inhibitor
Methot, Joey L.,Hoffman, Dawn Mampreian,Witter, David J.,Stanton, Matthew G.,Harrington, Paul,Hamblett, Christopher,Siliphaivanh, Phieng,Wilson, Kevin,Hubbs, Jed,Heidebrecht, Richard,Kral, Astrid M.,Ozerova, Nicole,Fleming, Judith C.,Wang, Hongmei,Szewczak, Alexander A.,Middleton, Richard E.,Hughes, Bethany,Cruz, Jonathan C.,Haines, Brian B.,Chenard, Melissa,Kenific, Candia M.,Harsch, Andreas,Secrist, J. Paul,Miller, Thomas A.
, p. 340 - 345 (2014/05/06)
The identification and in vitro and in vivo characterization of a potent SHI-1:2 are described. Kinetic analysis indicated that biaryl inhibitors exhibit slow binding kinetics in isolated HDAC1 and HDAC2 preparations. Delayed histone hyperacetylation and
SUBSTITUTED NICOTINAMIDE COMPOUNDS
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Page/Page column 22, (2009/05/29)
The present invention relates to a novel class of substituted nicotinamides. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplasti
Inhibitors of Histone Deacetylase
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Page/Page column 29-30, (2008/12/07)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseas
The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors
Hamblett, Christopher L.,Methot, Joey L.,Mampreian, Dawn M.,Sloman, David L.,Stanton, Matthew G.,Kral, Astrid M.,Fleming, Judith C.,Cruz, Jonathan C.,Chenard, Melissa,Ozerova, Nicole,Hitz, Anna M.,Wang, Hongmei,Deshmukh, Sujal V.,Nazef, Naim,Harsch, Andreas,Hughes, Bethany,Dahlberg, William K.,Szewczak, Alex A.,Middleton, Richard E.,Mosley, Ralph T.,Secrist, J. Paul,Miller, Thomas A.
, p. 5300 - 5309 (2008/03/14)
This communication highlights the development of a nicotinamide series of histone deacetylase inhibitors within the benzamide structural class. Extensive exploration around the nicotinamide core led to the discovery of a class I selective HDAC inhibitor that possesses excellent intrinsic and cell-based potency, acceptable ancillary pharmacology, favorable pharmacokinetics, sustained pharmacodynamics in vitro, and achieves in vivo efficacy in an HCT116 xenograft model.
Spirocyclic compounds
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Page/Page column 27-28; 31, (2008/06/13)
The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of n
SUBSTITUTED NICOTINAMIDE COMPOUNDS
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Page/Page column 50, (2010/11/27)
The present invention relates to a novel class of substituted nicotinamides.. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplast
ARYL-FUSED SPIROCYCLIC COMPOUNDS
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Page/Page column 49, (2008/06/13)
The present invention relates to a novel class of aryl-fused spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of ne
Substituted N-(2-aminophenyl)-benzamides, (E)-N-(2-aminophenyl)-acrylamides and their analogues: Novel classes of histone deacetylase inhibitors
Moradei, Oscar,Leit, Silvana,Zhou, Nancy,Frechette, Sylvie,Paquin, Isabelle,Raeppel, Stephane,Gaudette, Frederic,Bouchain, Giliane,Woo, Soon H.,Vaisburg, Arkadii,Fournel, Marielle,Kalita, Ann,Lu, Aihua,Trachy-Bourget, Marie-Claude,Yan, Pu T.,Liu, Jianhong,Li, Zuomei,Rahil, Jubrail,MacLeod, A. Robert,Besterman, Jeffrey M.,Delorme, Daniel
, p. 4048 - 4052 (2007/10/03)
Inhibition of histone deacetylases (HDACs) is emerging as a new strategy in human cancer therapy. Novel 2-aminophenyl benzamides and acrylamides, that can inhibit human HDAC enzymes and induce hyperacetylation of histones in human cancer cells, have been
