Synthesis and in vitro antitumor activity of 4(3H)-quinazolinone derivatives bearing dithiocarbamate chains / 药学学报
Acta Pharmaceutica Sinica
;
(12): 741-746, 2007.
Article
Dans Chinois
| WPRIM
| ID: wpr-268586
ABSTRACT
A series of 4(3H)-quinazolinone derivatives bearing dithiocarbamate side chains have been synthesized through the reaction of 6-bromomethyl-2-methyl-4(3H)-quinazolinone with CS2 and various amines in the presence of anhydrous K3PO4, and their structures were confirmed with ESI-MS, H NMR, elemental analysis or HRMS. The target compounds 8a -8q were tested for their in vitro antitumor activity against human myelogenous leukaemia K562 and human Hela cell lines by means of colorimetric MTT assay. Among the tested compounds, 8q exhibited in vitro inhibitory activity against K562 and Hela cells with IC50 values of 0.5 and 12.0 micromol x L(-01), respectively. Therefore, compound 8q is worthy to be a lead compound for the design and synthesis of new antitumor agents.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Relation structure-activité
/
Cellules HeLa
/
Structure moléculaire
/
Chimie
/
Cellules K562
/
Concentration inhibitrice 50
/
Éthylène-bis(dithiocarbamates)
/
Quinazolinones
/
Antinéoplasiques
Limites du sujet:
Humains
langue:
Chinois
Texte intégral:
Acta Pharmaceutica Sinica
Année:
2007
Type:
Article
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