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1 2009

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Pochodne akrydyny/akrydonu - synteza, aktywność biologiczna i zastosowanie kliniczne

Dzierzbicka K., Kawzowicz A., Koc A., Kukowska-Kaszuba M.

Wiadomości Chemiczne

2009

[Z] 63, 1-2

107-139

Nowadays the battle with tumor diseases and bacterial infections is an important test for the scientists. Therefore a lot of attention is focused on obtaining novel, more effective, selectively acting and less toxic drugs. Because of that reason, compounds with wide range of action like acridines/acridones are of great interest for scientists. This study contains synthesis and biological activity of acridine/acridone derivatives which are used in medicine as an antitumor agents and those which are at clinical trials. Among the synthetic methods there are modifications of Ullmann synthesis [2, 3, 9]. Lately Belmont et al. [11, 12] described a new methodology for the synthesis of 1,3,7-trisubstituted acridines, 1-amino-acridine and tetrahydro-cyclopenta[c]acridine-2,5-diones (Scheme 5). The starting materials are commercially available quinolines. Among acridine/acridone group there are compounds with diffe-rent molecular targets, e.g. topoisomerase inhibitors [1, 19-33], telomerase inhibitors [1, 34], protein-kinases inhibitors [36-40], P-glycoproteine inhibitors [56, 57, 76], conjugates with metals [1] and hypoxia-selective derivatives [2, 41-55]. This paper also describes compounds useful in Alzheimer disease [5, 16], antibacterial [2, 5], antiparasites [4, 5] and antiviral infections [5, 13, 14].