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rdf:type |
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lifeskim:mentions |
umls-concept:C0006826,
umls-concept:C0205177,
umls-concept:C0205460,
umls-concept:C0205531,
umls-concept:C0220781,
umls-concept:C0220825,
umls-concept:C0226896,
umls-concept:C0242640,
umls-concept:C0243071,
umls-concept:C0442027,
umls-concept:C0450442,
umls-concept:C1175773,
umls-concept:C1527415,
umls-concept:C1883254
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pubmed:issue |
18
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pubmed:dateCreated |
2004-8-24
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pubmed:abstractText |
Three novel taxinine analogues were prepared and tested for their activity as multidrug resistance (MDR) reversal agents in comparison with verapamil. In vitro testing demonstrated that compounds 8-10 possess MDR-reversal activity in the KB/V cell line. Half-hour after treatment with 5, 10, and 20 micromol/L compound 9, the intracellular rhodamine123 concentration increased 2.3, 2.9, and 3.2-fold, respectively, higher than 1.88-fold of 10 micromol/L verapamil in KB/V cell line. In vivo studies with VCR-resistant KB/V tumor xenografts showed that compound 9 in combination with VCR significantly inhibited tumor growth. Treatment with VCR or 9 alone did not result in growth inhibition. These results reveal that three taxinine analogues are good modifiers of MDR in tumor cells.
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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 |
Sep
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
20
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pubmed:volume |
14
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4767-70
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15324905-Administration, Oral,
pubmed-meshheading:15324905-Animals,
pubmed-meshheading:15324905-Antineoplastic Agents,
pubmed-meshheading:15324905-Carcinoma, Squamous Cell,
pubmed-meshheading:15324905-Cell Line, Tumor,
pubmed-meshheading:15324905-Cell Survival,
pubmed-meshheading:15324905-Dose-Response Relationship, Drug,
pubmed-meshheading:15324905-Drug Resistance, Multiple,
pubmed-meshheading:15324905-Drug Resistance, Neoplasm,
pubmed-meshheading:15324905-Humans,
pubmed-meshheading:15324905-Mice,
pubmed-meshheading:15324905-Mice, Nude,
pubmed-meshheading:15324905-Taxoids,
pubmed-meshheading:15324905-Time Factors,
pubmed-meshheading:15324905-Vincristine,
pubmed-meshheading:15324905-Xenograft Model Antitumor Assays
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pubmed:year |
2004
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pubmed:articleTitle |
Synthesis and biological evaluation of taxinine analogues as orally active multidrug resistance reversal agents in cancer.
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pubmed:affiliation |
Department of Pharmacology, Institute of Materia Medica, Chinese Academic of Medical Science and Peking Union Medical College, 1 Xian Nong Tan Street, Beijng 100050, China.
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pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, Non-U.S. Gov't
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