Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
16
|
pubmed:dateCreated |
1993-9-24
|
pubmed:abstractText |
The synthesis and thymidylate synthase (TS) inhibitory activity of a series of simple benzo[f]-quinazolin-1(2H)-ones are described. Fully aromatic 3-amino compounds with compact lipophilic substituents in the 9-position were found to have I50 values as low as 20 nM on the isolated enzyme, and represent the first examples of potent, folate-based TS inhibitors that completely lack any structural feature corresponding to the (p-aminobenzoyl)glutamate moiety of the cofactor. A number of the compounds also showed moderate growth inhibitory activity against a human colon adenocarcinoma cell line (SW480), with IC50 values as low as 2 microM.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
Aug
|
pubmed:issn |
0022-2623
|
pubmed:author | |
pubmed:issnType |
Print
|
pubmed:day |
6
|
pubmed:volume |
36
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
2279-91
|
pubmed:dateRevised |
2004-11-17
|
pubmed:meshHeading |
pubmed-meshheading:8360872-Adenocarcinoma,
pubmed-meshheading:8360872-Cell Division,
pubmed-meshheading:8360872-Colonic Neoplasms,
pubmed-meshheading:8360872-Escherichia coli,
pubmed-meshheading:8360872-Humans,
pubmed-meshheading:8360872-Quinazolines,
pubmed-meshheading:8360872-Structure-Activity Relationship,
pubmed-meshheading:8360872-Thymidylate Synthase,
pubmed-meshheading:8360872-Tumor Cells, Cultured
|
pubmed:year |
1993
|
pubmed:articleTitle |
Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some 3-amino- and 3-methylbenzo[f]quinazolin-1(2H)-ones.
|
pubmed:affiliation |
Wellcome Research Laboratories, Research Triangle Park, North Carolina 27709.
|
pubmed:publicationType |
Journal Article
|