Source:http://linkedlifedata.com/resource/pubmed/id/15049616
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
7
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pubmed:dateCreated |
2004-3-30
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pubmed:abstractText |
Aaptamine (1) was used as starting material for synthetic transformation to isoaaptamine (2), 9-demethylaaptamine (5), and 4-methylaaptamine (6). A general method for the selective O-demethylation of such 1H-benzo[de][1,6]-naphthyridine (1) marine sponge constituents at position C-9 has been developed. Selective O-demethylation of aaptamine (1) and 1-methylaaptamine (11) with 48% hydrobromic acid led to 9-demethylaaptamine (5) and isoaaptamine (2), respectively. A selection of other aaptamine derivatives were synthesized, and their structures were unambiguously determined by X-ray methods. In addition, their cancer cell growth inhibitory properties were evaluated against the murine P388 lymphocytic cell line and a minipanel of human cancer cell lines. Evaluation as inhibitors of the PKC signal transduction pathway and against a selection of microorganisms was also undertaken. Aaptamine derivatives 3 and 5 had broad-spectrum antimicrobial activities.
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pubmed:grant | |
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 |
Apr
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pubmed:issn |
0022-3263
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pubmed:author |
pubmed-author:BlumbergPeter MPM,
pubmed-author:HamelErnestE,
pubmed-author:HeraldDelbert LDL,
pubmed-author:HiggsKerianne CKC,
pubmed-author:HoffmannHolgerH,
pubmed-author:KnightJohn CJC,
pubmed-author:LewinNancy ENE,
pubmed-author:McNultyJamesJ,
pubmed-author:MurphyAlisonA,
pubmed-author:PearceLarry VLV,
pubmed-author:PettitGeorge RGR,
pubmed-author:PettitRobin KRK
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pubmed:issnType |
Print
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pubmed:day |
2
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pubmed:volume |
69
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2251-6
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:15049616-Animals,
pubmed-meshheading:15049616-Antineoplastic Agents,
pubmed-meshheading:15049616-Bacteria,
pubmed-meshheading:15049616-Candida albicans,
pubmed-meshheading:15049616-Cryptococcus neoformans,
pubmed-meshheading:15049616-Drug Screening Assays, Antitumor,
pubmed-meshheading:15049616-Leukemia P388,
pubmed-meshheading:15049616-Mice,
pubmed-meshheading:15049616-Microbial Sensitivity Tests,
pubmed-meshheading:15049616-Molecular Structure,
pubmed-meshheading:15049616-Naphthyridines,
pubmed-meshheading:15049616-Porifera,
pubmed-meshheading:15049616-Structure-Activity Relationship,
pubmed-meshheading:15049616-Tumor Cells, Cultured
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pubmed:year |
2004
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pubmed:articleTitle |
Antineoplastic agents 491. Synthetic conversion of aaptamine to isoaaptamine, 9-demethylaaptamine, and 4-methylaaptamine.
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pubmed:affiliation |
Cancer Research Institute and Department of Chemistry and Biochemistry, Arizona State University, P.O. Box 872404, Tempe, Arizona 85287-2404, USA.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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