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  • Title: Synthesis and antiproliferative properties of 4-aminoquinazoline derivatives as inhibitors of EGF receptor-associated tyrosine kinase activity.
    Author: Bouey-Bencteux E, Loison C, Pommery N, Houssin R, Hénichart JP.
    Journal: Anticancer Drug Des; 1998 Dec; 13(8):893-922. PubMed ID: 10335266.
    Abstract:
    The mitogenic action of EGF is mediated by ligand-induced autophosphorylation of the EGF receptor (EGF-R), which is commonly overexpressed in numerous human cancers. Inhibitors of receptor tyrosine kinase (RTK) activity could therefore be considered as effective potential antitumor agents. For this purpose, 4-aminoquinazoline derivatives were prepared and evaluated for their ability to inhibit RTK activity and the autophosphorylation of EGF-R. In addition, these compounds were tested on A431 cell growth to estimate their antiproliferative effect. The results showed that the substituent at the 4-position of the quinazoline ring must be an aromatic amine carrying small lipophilic electron-withdrawing groups on the 3- (or 2-) position of the phenyl ring. This aromatic moiety might be far from the quinazoline provided that the linking group is conformationally restricted, such as with piperazine. Hydrophilic and non-aromatic substituents such as morpholine gave completely inactive compounds. Introduction of a bulk at the 2-position of the quinazoline ring in 2,4-diaminoquinazolines or tricyclic compounds led to inactive products. This study reports additional structure-activity relationships of a well-characterized series to develop new inhibitors of EGF-R-associated tyrosine kinase activity.
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