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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2009-2-16
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pubmed:abstractText |
The successful application of both solid and solution phase library synthesis, combined with tight integration into the medicinal chemistry effort, resulted in the efficient optimization of a novel structural series of selective HDAC1/HDAC2 inhibitors by the MRL-Boston Parallel Medicinal Chemistry group. An initial lead from a small parallel library was found to be potent and selective in biochemical assays. Advanced compounds were the culmination of iterative library design and possess excellent biochemical and cellular potency, as well as acceptable PK and efficacy in animal 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:BerkScott CSC,
pubmed-author:ChenardMelissaM,
pubmed-author:CruzJonathan CJC,
pubmed-author:DahlbergWilliam KWK,
pubmed-author:FlemingJudith CJC,
pubmed-author:HamillJulie EJE,
pubmed-author:HarschAndreasA,
pubmed-author:HughesBethanyB,
pubmed-author:KattarSolomon DSD,
pubmed-author:KenificCandia MCM,
pubmed-author:KralAstrid MAM,
pubmed-author:MethotJoey LJL,
pubmed-author:MiddletonRichard ERE,
pubmed-author:MillerThomas ATA,
pubmed-author:OzerovaNicoleN,
pubmed-author:SecristPaulP,
pubmed-author:SurdiLaura MLM,
pubmed-author:SzewczakAlexander AAA,
pubmed-author:TempestPaulP,
pubmed-author:WangHongmeiH,
pubmed-author:ZabierekAnnaA
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pubmed:issnType |
Electronic
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pubmed:day |
15
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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 |
1168-72
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:19138845-Animals,
pubmed-meshheading:19138845-Combinatorial Chemistry Techniques,
pubmed-meshheading:19138845-Dogs,
pubmed-meshheading:19138845-Drug Design,
pubmed-meshheading:19138845-Histone Deacetylase 1,
pubmed-meshheading:19138845-Histone Deacetylase 2,
pubmed-meshheading:19138845-Histone Deacetylase Inhibitors,
pubmed-meshheading:19138845-Humans,
pubmed-meshheading:19138845-Molecular Structure,
pubmed-meshheading:19138845-Rats,
pubmed-meshheading:19138845-Repressor Proteins,
pubmed-meshheading:19138845-Structure-Activity Relationship,
pubmed-meshheading:19138845-Xenograft Model Antitumor Assays
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pubmed:year |
2009
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pubmed:articleTitle |
Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.
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pubmed:affiliation |
Department of Drug Design and Optimization, Merck Research Laboratories, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. sam_kattar@merck.com
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pubmed:publicationType |
Journal Article
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