rdf:type |
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lifeskim:mentions |
|
pubmed:issue |
9
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pubmed:dateCreated |
2007-4-2
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pubmed:abstractText |
A series of aryl- and aroyl-substituted chalcone analogues of the tubulin binding agent combretastatin A4 (1) were prepared, using a recently introduced one-pot palladium-mediated hydrostannylation-coupling reaction sequence. These chalcones were converted to indanones by Nazarov cyclisation, followed by oxidation to give the corresponding indenones. Indenones were also prepared using a palladium-mediated formal [3+2]-cycloaddition process between ortho-halobenzaldehydes and diarylpropynones. All compounds were assessed as inhibitors of tubulin polymerisation, but only E-31 had activity similar to that of 1. However, compound E-31 did not exhibit antiproliferative activity against the MCF-7 cell line.
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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
|
pubmed:month |
May
|
pubmed:issn |
0968-0896
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
1
|
pubmed:volume |
15
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
3290-8
|
pubmed:dateRevised |
2007-12-3
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pubmed:meshHeading |
pubmed-meshheading:17360188-Animals,
pubmed-meshheading:17360188-Brain,
pubmed-meshheading:17360188-Cattle,
pubmed-meshheading:17360188-Cell Line, Tumor,
pubmed-meshheading:17360188-Cell Proliferation,
pubmed-meshheading:17360188-Chalcone,
pubmed-meshheading:17360188-Drug Screening Assays, Antitumor,
pubmed-meshheading:17360188-Humans,
pubmed-meshheading:17360188-Indans,
pubmed-meshheading:17360188-Indenes,
pubmed-meshheading:17360188-Molecular Structure,
pubmed-meshheading:17360188-Stereoisomerism,
pubmed-meshheading:17360188-Stilbenes,
pubmed-meshheading:17360188-Structure-Activity Relationship,
pubmed-meshheading:17360188-Tubulin
|
pubmed:year |
2007
|
pubmed:articleTitle |
The concise synthesis of chalcone, indanone and indenone analogues of combretastatin A4.
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pubmed:affiliation |
Department of Medicinal Chemistry, Faculty of Pharmacy, Monash University, 381 Royal Pde, Parkville, Australia.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
|