engleski

The novel coumarin[3, 2-c]thiophene and its hydroxamic acid and ureido derivatives : synthesis and cytostatic activity evaluations

In the present paper, we report on the synthesis and in vitro anti-tumour effects of novel hydroxamic acid (compounds 4 and 5) and ureido (compounds 7-11) derivatives containing coumarin[3, 2-c]thiophene moiety. The results of anti-proliferative assays performed on a panel of selected human tumour cell lines revealed stronger concentration-dependent anti-proliferative activity of coumarin[3, 2-c]thiophene (7-11) ureido derivatives in comparison with coumarin[3, 2-c]thiophene hydroxamic acid derivatives (4 and 5). Nevertheless, compounds 7-10 were cytotoxic on normal human fibroblasts as well. Importantly, the ureido derivative 11 and hydroxamic acid derivatives 4 and 5 showed pronounced and selective inhibitory activity towards cervical carcinoma (HeLa) cell line with concomitant low or no cytotoxicity on normal human fibroblasts. These compounds can therefore be considered as potential anti-tumour lead compounds for further structural optimization.

coumarin[3; 2-c]thiophene; urea; hydroxamic acid; antitumour

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