Linked Life Data

7097545

Source:http://linkedlifedata.com/resource/pubmed/id/7097545

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6
pubmed:dateCreated
1982-9-24
pubmed:abstractText
The synthesis of 4-amino-4-deoxy-N10-methylpteroyl-(6-diazo-5-oxo)-L-norleucine and 4-amino-4-deoxy-N10-methylpteroyl-(6-chloro-5-oxo)-L-norleucine, analogs of methotrexate in which the gamma-carboxyl group is replaced by a diazoketone and a chloromethylketone, respectively, was carried out. The analogs inhibited the growth of leukemia L-1210 cells in culture by 50% at 4 X 10(-7) M and 2 X 10(-7) M, respectively, and were effective inhibitors of the synthesis of thymidylate in L-1210 cells in vitro (I50 = 3 X 10(-6) M), exhibiting significant antifolate activity. The results demonstrated the feasibility of introducing chemically reactive groups at the gamma-position of pteroyl glutamates with retention of biological activity. However, in the systems investigated thus far, there was no evidence of covalent bond formation due to these reactive groups at the active sites of the enzymes.
pubmed:grant
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0022-3549
pubmed:author
pubmed:issnType
Print
pubmed:volume
71
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
717-9
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed:year
1982
pubmed:articleTitle
Diazoketone and chloromethylketone analogs of methotrexate as potential antitumor agents.
pubmed:publicationType
Journal Article, Research Support, U.S. Gov't, P.H.S.