Linked Life Data

2951522

Source:http://linkedlifedata.com/resource/pubmed/id/2951522

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1987-5-11
pubmed:abstractText
A synthesis of 5-chloro- and 5-fluoro-1-(2'-fluoro-2'-deoxy-beta-D-ribofuranosyl)uracil (4a and 4b) and their 2-14C analogues has been developed. The tissue distribution of these radiolabeled compounds in BDF1 mice bearing Lewis lung tumors has been investigated. Compounds 4a and 4b undergo rapid blood clearance and urinary excretion. Selective retention of radioactivity was observed in tumor tissue, spleen, and intestine and with compound 4b also in the bone. Maximum tumor to blood ratios of 4.2 for the 5-chloro compound 4a and 10.3 for the 5-fluoro compound 4b were observed at 4h. These compounds were resistant to phosphorylytic cleavage and dehalogenation as indicated by the metabolic products observed in the urine and the absence of radioactivity in the liver. The interaction of 4b with the mouse erythrocyte transporter system was compared with physiological nucleosides in respect to ability to effect zero-trans influx of thymidine. The results show a competitive inhibition between 4b and the natural nucleoside. Evidence is presented for the direct metabolic defluorination of 5-fluorouracil to form uracil.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
30
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
670-5
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Synthesis and tumor uptake of 5-halo-1-(2'-fluoro-2'-deoxy-beta-D-ribofuranosyl)[2-14C]uracils.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't