rdf:type |
|
lifeskim:mentions |
|
pubmed:issue |
24
|
pubmed:dateCreated |
1994-1-11
|
pubmed:abstractText |
The synthesis of a series of 2-arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and 2-amino-4-(isothiocyanatomethyl)selenazole is described. In vitro antiproliferative evaluations were carried out using L1210 cells. The 2-(alkylamido)thiazole derivatives were moderately antiproliferative, with IC50's of 4-8 microM. A significant increase in activity was obtained for the arylamido derivatives, with IC50's of 0.2-1 microM. The results obtained for the selenazoles were similar to those for the thiazoles. 2-Benzamido-4-(isothiocyanatomethyl)-thiazole (19) was found to be a potent inhibitor of GMP synthetase. None of the compounds prepared in this study demonstrated antifilarial activity.
|
pubmed:grant |
|
pubmed:language |
eng
|
pubmed:journal |
|
pubmed:citationSubset |
IM
|
pubmed:chemical |
|
pubmed:status |
MEDLINE
|
pubmed:month |
Nov
|
pubmed:issn |
0022-2623
|
pubmed:author |
|
pubmed:issnType |
Print
|
pubmed:day |
26
|
pubmed:volume |
36
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
3849-52
|
pubmed:dateRevised |
2007-11-14
|
pubmed:meshHeading |
pubmed-meshheading:8254615-Animals,
pubmed-meshheading:8254615-Antineoplastic Agents,
pubmed-meshheading:8254615-Carbon-Nitrogen Ligases,
pubmed-meshheading:8254615-Cell Division,
pubmed-meshheading:8254615-Filaricides,
pubmed-meshheading:8254615-Isothiocyanates,
pubmed-meshheading:8254615-Leukemia L1210,
pubmed-meshheading:8254615-Ligases,
pubmed-meshheading:8254615-Mitosis,
pubmed-meshheading:8254615-Mitotic Index,
pubmed-meshheading:8254615-Molecular Structure,
pubmed-meshheading:8254615-Selenium Compounds,
pubmed-meshheading:8254615-Structure-Activity Relationship,
pubmed-meshheading:8254615-Thiazoles
|
pubmed:year |
1993
|
pubmed:articleTitle |
Synthesis of 2,4-disubstituted thiazoles and selenazoles as potential antifilarial and antitumor agents. 2. 2-Arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and 2-amino-4-(isothiocyanatomethyl)selenazole.
|
pubmed:affiliation |
Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Ann Arbor 48109-1065.
|
pubmed:publicationType |
Journal Article,
Comparative Study,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
|