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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 |
2008-2-7
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pubmed:abstractText |
We report a series of novel inhibitors of protein farnesyltransferase based on the 2-oxotetrahydroquinoline scaffold. We developed an efficient synthesis of these compounds. These compounds show selective inhibtion of the malaria versus human farnesyltransferase and inhibit the growth of the malaria parasite in the low nanomolar range. Some of the compounds are at least an order of magnitude more stable to metabolic degradation than the corresponding tetrahydroquinolines.
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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 |
0022-2623
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pubmed:author |
|
|
pubmed:issnType |
Print
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pubmed:day |
14
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pubmed:volume |
51
|
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pubmed:owner |
NLM
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|
pubmed:authorsComplete |
Y
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pubmed:pagination |
384-7
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pubmed:dateRevised |
2008-5-20
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pubmed:meshHeading |
pubmed-meshheading:18198825-Alkyl and Aryl Transferases,
pubmed-meshheading:18198825-Animals,
pubmed-meshheading:18198825-Antimalarials,
pubmed-meshheading:18198825-Crystallography, X-Ray,
pubmed-meshheading:18198825-Drug Stability,
pubmed-meshheading:18198825-Humans,
pubmed-meshheading:18198825-Mice,
pubmed-meshheading:18198825-Microsomes, Liver,
pubmed-meshheading:18198825-Models, Molecular,
pubmed-meshheading:18198825-Molecular Structure,
pubmed-meshheading:18198825-Plasmodium falciparum,
pubmed-meshheading:18198825-Quinolines,
pubmed-meshheading:18198825-Rats,
pubmed-meshheading:18198825-Structure-Activity Relationship
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pubmed:year |
2008
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|
pubmed:articleTitle |
2-Oxotetrahydroquinoline-based antimalarials with high potency and metabolic stability.
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pubmed:affiliation |
Departments of Chemistry, Medicine, and Biochemistry, University of Washington, Seattle, Washington 98195. gelb@chem.washington.edu.
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pubmed:publicationType |
Journal Article,
In Vitro
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