Source:http://linkedlifedata.com/resource/pubmed/id/19846303
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
23
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pubmed:dateCreated |
2009-11-5
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pubmed:abstractText |
A series of maslinic acid derivatives have been synthesized by introducing various fused heterocyclic rings at C-2 and C-3 positions. Their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Most of the compounds exhibited a dramatic increase in inhibitory potency and selectivity, the two most potent PTP1B inhibitors 20 (IC(50)=0.61 microM) and 29 (IC(50)=0.64 microM) showed about 10-fold more potent than lead compound maslinic acid. More importantly, 29 possesses the best selectivity of 6.9-fold for PTP1B over TCPTP.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Dec
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pubmed:issn |
1464-3405
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pubmed:author | |
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 |
6618-22
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pubmed:meshHeading |
pubmed-meshheading:19846303-Dose-Response Relationship, Drug,
pubmed-meshheading:19846303-Drug Design,
pubmed-meshheading:19846303-Enzyme Inhibitors,
pubmed-meshheading:19846303-Molecular Conformation,
pubmed-meshheading:19846303-Protein Tyrosine Phosphatase, Non-Receptor Type 1,
pubmed-meshheading:19846303-Stereoisomerism,
pubmed-meshheading:19846303-Structure-Activity Relationship,
pubmed-meshheading:19846303-Triterpenes
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pubmed:year |
2009
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pubmed:articleTitle |
Synthesis and biological evaluation of heterocyclic ring-substituted maslinic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.
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pubmed:affiliation |
Institute of Medicinal Chemistry, Department of Chemistry, East China Normal University, Shanghai 200062, China.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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