rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
12
|
pubmed:dateCreated |
2002-12-27
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pubmed:abstractText |
A series of 12 semisynthetic discodermolide analogues, 2-13, have been prepared using natural (+)-discodermolide (1) and evaluated for in vitro cytotoxicity against cultured murine P-388 leukemia and A-549 human adenocarcinoma cells. These semisynthetic analogues showed a significant variation of cytotoxicity and confirmed the importance of the C-7 through C-19 molecular fragment for potency. Specifically, these analogues suggested the importance of the C-11 and C-17 hydroxyl groups and the C-13 double bond for the potency of discodermolide. The preparation, structure elucidation, and biological activity of these new analogues are described.
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pubmed:grant |
|
pubmed:language |
eng
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pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Dec
|
pubmed:issn |
0163-3864
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:volume |
65
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
1830-7
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:12502323-Adenocarcinoma,
pubmed-meshheading:12502323-Alkanes,
pubmed-meshheading:12502323-Animals,
pubmed-meshheading:12502323-Antineoplastic Agents,
pubmed-meshheading:12502323-Carbamates,
pubmed-meshheading:12502323-Drug Screening Assays, Antitumor,
pubmed-meshheading:12502323-Humans,
pubmed-meshheading:12502323-Lactones,
pubmed-meshheading:12502323-Leukemia P388,
pubmed-meshheading:12502323-Mice,
pubmed-meshheading:12502323-Microtubules,
pubmed-meshheading:12502323-Molecular Structure,
pubmed-meshheading:12502323-Nuclear Magnetic Resonance, Biomolecular,
pubmed-meshheading:12502323-Porifera,
pubmed-meshheading:12502323-Pyrones,
pubmed-meshheading:12502323-Structure-Activity Relationship,
pubmed-meshheading:12502323-Tumor Cells, Cultured
|
pubmed:year |
2002
|
pubmed:articleTitle |
Semisynthetic analogues of the microtubule-stabilizing agent discodermolide: preparation and biological activity.
|
pubmed:affiliation |
Division of Biomedical Marine Research, Harbor Branch Oceanographic Institution, 5600 U.S. 1 North, Fort Pierce, FL 34946, USA. sgunaseker@hboi.edu
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.
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