Linked Life Data

17069934

Source:http://linkedlifedata.com/resource/pubmed/id/17069934

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
2007-2-26
pubmed:abstractText
Two 4-methylideneisoxazolidin-5-ones (4a,b), which are alpha-methylidene-gamma-lactones containing a nitrogen atom in the lactone ring, were synthesized. Their cytotoxic properties were evaluated against promyelocytic leukemia HL-60 cells. Both 4a and 4b exhibited relatively high cytotoxic activity with an IC(50) of 4.1 and 5.4 microM, respectively. Caspase-3 activity assay revealed that both isoxazolidinones (4) were able to induce apoptosis process in time- and concentration-dependent manner. Using multiplex PCR analysis, it was observed that 4 caused distinct inhibition of BCL-2 gene expression. Expression of BAX, a pro-apoptotic gene remained unchanged. It was also found that 4a,b did not induce the expression of MDR1 and MRP1 genes, related to multidrug resistance. In addition, cytotoxicity data obtained for drug-sensitive and drug-resistant HL-60 ADR cells revealed that the investigated compounds were poor substrates for transport by MRP1 efflux pump, suggesting that they might be useful for treating drug-resistant tumors. Furthermore, antimicrobial properties of 4a,b were evaluated. They showed significant activity against fungi Candida albicans, but only a weak activity against all tested Gram-positive and Gram-negative bacterial strains.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Feb
pubmed:issn
0223-5234
pubmed:author
pubmed:issnType
Print
pubmed:volume
42
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
248-55
pubmed:meshHeading
pubmed:year
2007
pubmed:articleTitle
Synthesis and biological evaluation of 4-methylideneisoxazolidin-5-ones--a new class of highly cytotoxic alpha-methylidene-gamma-lactones.
pubmed:affiliation
Department of Pharmaceutical Biochemistry, Medical University of ?ód?, Muszy?skiego 1, 90-151 ?ód?, Poland. mrozalsk@csk.umed.lodz.pl <mrozalsk@csk.umed.lodz.pl>
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't