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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2009-3-16
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pubmed:abstractText |
We have recently reported on a novel class of histone deacetylase (HDAC) inhibitors bearing a sulfamide group as the zinc-binding unit. Herein, we report on the synthesis of sulfamide based inhibitors designed around a lysine scaffold and their structure-activity relationships against HDAC1 and HDAC6 isotypes as well as 293T cells. Our efforts led us to an improvement of the originally disclosed lysine-based sulfamide, 2a to compound 12h which has equal potency in enzyme and cell-based assays as well as enhanced metabolic stability and PK profile.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:AjamianAlainA,
pubmed-author:AllanMartinM,
pubmed-author:BestermanJeffrey MJM,
pubmed-author:DézielRobertR,
pubmed-author:FournelMarielleM,
pubmed-author:GuoTimT,
pubmed-author:LefebvreSylvainS,
pubmed-author:LiZuomeiZ,
pubmed-author:MankuSukhdevS,
pubmed-author:NguyenNatalieN,
pubmed-author:NicolescuAlinaA,
pubmed-author:PetschnerAndrea JAJ,
pubmed-author:RahilJubrailJ,
pubmed-author:RodrigueJacquesJ,
pubmed-author:TherrienEricE,
pubmed-author:WahhabAmalA,
pubmed-author:WangJamesJ
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
19
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1866-70
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:19272776-Animals,
pubmed-meshheading:19272776-Benzimidazoles,
pubmed-meshheading:19272776-Carrier Proteins,
pubmed-meshheading:19272776-Cell Line,
pubmed-meshheading:19272776-Enzyme Inhibitors,
pubmed-meshheading:19272776-Histone Deacetylase Inhibitors,
pubmed-meshheading:19272776-Histone Deacetylases,
pubmed-meshheading:19272776-Humans,
pubmed-meshheading:19272776-Lysine,
pubmed-meshheading:19272776-Protein Isoforms,
pubmed-meshheading:19272776-Rats,
pubmed-meshheading:19272776-Structure-Activity Relationship,
pubmed-meshheading:19272776-Sulfonamides
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pubmed:year |
2009
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pubmed:articleTitle |
Synthesis and evaluation of lysine derived sulfamides as histone deacetylase inhibitors.
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pubmed:affiliation |
MethylGene Inc., Departments of Medicinal Chemistry, 7220 rue Frederick-Banting, Montreal, Quebec, Canada H4S 2A1.
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pubmed:publicationType |
Journal Article
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