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Monocyclic beta-lactam analogues as antitumor agents

It has been reported that some monocyclic beta-lactams exhibit antileukemic activity. The aim of this study was to investigate the potential antitumor activity of monocyclic b-lactam (4-oxoazetidin) analogues. Monocyclic beta-lactam analogues were prepared by chemical transformation of some penicillin derivatives. Their antitumor activity were examined in human tissue cultured cell lines. Several of these compounds showed significant antitumor effect in vitro depending on the concentration and the tumor type. The best inhibitory effect was achieved with the compound 2-[(2RS)-3, 3-dibromo-2-chloro-4-oxo-azetidin-1-yl]-3-methyl-but-2-enoic acid (14). In vitro experiments on human tumor cell lines showed that antitumor effect depends on the substituents on oxazetidine ring. Thus, halo substituents contributed that compounds 14 and 15 exhibited the best antitumor effect. These compounds almost completely arrested the growth of MiaPaCa2 cells and had a strong inhibitory effect on the growth of other examined cell lines.

antitumor activity ; monocyclic beta-lactam analogues (4-oxoazetidine) ; human tumor cell lines

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