Source:http://linkedlifedata.com/resource/pubmed/id/10937725
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
15
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pubmed:dateCreated |
2000-12-6
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pubmed:abstractText |
Two series of anhydride modified cantharidin analogues were synthesised and screened for their phosphatase inhibition (PP1 and PP2A) and cytotoxicity in various cancer cell lines (Ovarian A2780, ADDP; Osteosarcoma 143B; and Colon HCT116 and HT29). One series was synthesised by a novel, high yielding one-pot hydrogenation-ring-opening-esterification procedure, the other by acid catalysed acetal formation. Analogues 5-7 and 9 displayed moderate PP2A selectivity (ca. 5- to 20-fold) and inhibition typically in the low microM range (comparable, in some cases to cantharidin). The anticancer activity of these analogues varied with the cell line under study; however, many of them showed selective cytotoxicity for the colon tumour cell lines.
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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/Anhydrides,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Cantharidin,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Isoenzymes,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphoprotein Phosphatases
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0960-894X
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
7
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pubmed:volume |
10
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1687-90
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pubmed:dateRevised |
2007-11-15
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pubmed:meshHeading |
pubmed-meshheading:10937725-Anhydrides,
pubmed-meshheading:10937725-Antineoplastic Agents,
pubmed-meshheading:10937725-Cantharidin,
pubmed-meshheading:10937725-Drug Screening Assays, Antitumor,
pubmed-meshheading:10937725-Enzyme Inhibitors,
pubmed-meshheading:10937725-Humans,
pubmed-meshheading:10937725-Isoenzymes,
pubmed-meshheading:10937725-Phosphoprotein Phosphatases,
pubmed-meshheading:10937725-Tumor Cells, Cultured
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pubmed:year |
2000
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pubmed:articleTitle |
Anhydride modified cantharidin analogues: synthesis, inhibition of protein phosphatases 1 and 2A and anticancer activity.
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pubmed:affiliation |
Medicinal Chemistry Group, School of Biological and Chemical Sciences, The University of Newcastle, Callaghan, NSW 2308, Australia. amcclusk@mail.newcastle.edu.au
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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