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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
2009-1-27
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pubmed:abstractText |
Analogues of the clinical compound MGCD0103 (A) were designed and synthesized. These compounds inhibit recombinant human HDAC1 with IC(50) values in the sub-micromolar range. In human cancer cells growing in culture these compounds induce hyperacetylation of histones, cause expression of the tumor suppressor protein p21(WAF1/CIP1), and inhibit cellular proliferation. Lead molecule of the series, compound 25 is metabolically stable, possesses favorable pharmacokinetic characteristics and is orally active in vivo in different mouse tumor xenograft models.
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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 |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BestermanJeffrey MJM,
pubmed-author:DelormeDanielD,
pubmed-author:FournelMarielleM,
pubmed-author:FréchetteSylvieS,
pubmed-author:GaudetteFrédéricF,
pubmed-author:IsakovicLjubomirL,
pubmed-author:KalitaAnnA,
pubmed-author:LaroucheGuillaumeG,
pubmed-author:LeitSilvanaS,
pubmed-author:LiZuomeiZ,
pubmed-author:LiuJianhongJ,
pubmed-author:LuAihuaA,
pubmed-author:MoradeiOscarO,
pubmed-author:MurakamiKojiK,
pubmed-author:PaquinIsabelleI,
pubmed-author:RaeppelStéphaneS,
pubmed-author:RahilJubrailJ,
pubmed-author:Trachy-BourgetMarie-ClaudeMC,
pubmed-author:VaisburgArkadiiA,
pubmed-author:WangJamesJ,
pubmed-author:YanPu TheresaPT,
pubmed-author:ZhouNancyN
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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 |
644-9
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pubmed:meshHeading |
pubmed-meshheading:19114304-Animals,
pubmed-meshheading:19114304-Antineoplastic Agents,
pubmed-meshheading:19114304-Benzamides,
pubmed-meshheading:19114304-Cell Line, Tumor,
pubmed-meshheading:19114304-Cell Proliferation,
pubmed-meshheading:19114304-Chemistry, Pharmaceutical,
pubmed-meshheading:19114304-Cyclin-Dependent Kinase Inhibitor p21,
pubmed-meshheading:19114304-Drug Design,
pubmed-meshheading:19114304-Enzyme Inhibitors,
pubmed-meshheading:19114304-Histone Deacetylase Inhibitors,
pubmed-meshheading:19114304-Humans,
pubmed-meshheading:19114304-Inhibitory Concentration 50,
pubmed-meshheading:19114304-Mice,
pubmed-meshheading:19114304-Neoplasm Transplantation,
pubmed-meshheading:19114304-Pyrimidines,
pubmed-meshheading:19114304-Structure-Activity Relationship
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pubmed:year |
2009
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pubmed:articleTitle |
SAR and biological evaluation of analogues of a small molecule histone deacetylase inhibitor N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide (MGCD0103).
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pubmed:affiliation |
MethylGene Inc., Department of Medicinal Chemistry, 7220 Frederick-Banting, Montréal, Que., Canada H4S 2A1. raeppels@methylgene.com
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pubmed:publicationType |
Journal Article
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