Source:http://linkedlifedata.com/resource/pubmed/id/21714538
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
15
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pubmed:dateCreated |
2011-8-4
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pubmed:abstractText |
Histone deacetylase (HDAC) has emerged as an attractive target for the development of antitumor agents during the past decade. Previously tetrahydroisoquinoline-bearing hydroxamic acid analogue, ZYJ-25e (1), was identified and validated as a potent histone deacetylase inhibitor (HDACi) with marked in vitro and in vivo antitumor potency. In the present study, further modification of 1 led to another more potent, orally active HDACi, ZYJ-34c (4). Compared to FDA-approved drug suberoylanilide hydroxamic acid (SAHA), compound 4 exhibited higher in vivo antitumor potency in a human breast carcinoma (MDA-MB-231) xenograft model and in a mouse hepatoma-22 (H22) pulmonary metastasis model and similar in vivo antitumor potency in a human colon tumor (HCT116) xenograft model.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Cytostatic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Histone Deacetylase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Hydroxamic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Isoquinolines,
http://linkedlifedata.com/resource/pubmed/chemical/vorinostat
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
1520-4804
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
11
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pubmed:volume |
54
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5532-9
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pubmed:meshHeading |
pubmed-meshheading:21714538-Animals,
pubmed-meshheading:21714538-Cell Line, Tumor,
pubmed-meshheading:21714538-Cytostatic Agents,
pubmed-meshheading:21714538-Female,
pubmed-meshheading:21714538-Histone Deacetylase Inhibitors,
pubmed-meshheading:21714538-Humans,
pubmed-meshheading:21714538-Hydroxamic Acids,
pubmed-meshheading:21714538-Isoquinolines,
pubmed-meshheading:21714538-Mice,
pubmed-meshheading:21714538-Xenograft Model Antitumor Assays
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pubmed:year |
2011
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pubmed:articleTitle |
Discovery of a tetrahydroisoquinoline-based hydroxamic acid derivative (ZYJ-34c) as histone deacetylase inhibitor with potent oral antitumor activities.
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pubmed:affiliation |
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, PR China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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