hrvatski

Heterociklički kondenzirani kinoloni i kinolini kao potencijalni antitumorski agensi

A lot of condensed benzothienoquinolones, benzothienonaphthyridones and thienothienylquinolones, as well as, benzimidazo[1, 2-a]quinolines and their heterocyclic analogues diazacyclopenta[c]fluorenes were prepared in multistep synthesis:The pharmacophore groups were introduced in the main structure. Amoung the lot of prepared compounds the best antitumor activities „in vitro“ on a few human tumor cell lines showed the compounds as follows: The change of the terminal benzene nuclei of the acidic part of the molecule with thiophene in quinolones didn’t significantly influenced on the antitumor activity, while the substitution of the quinolone nulei with the naphthyridone nuclei increased antitumor activity. Quinolones and quinolines showed very similar and good antitumor activity. DNA binding reactions were detected by changes in fluorescence, UV and CD spectra.

Heetrocyclic condensed quinolones; quinolines; antitumor activity

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