engleski

Synthesis and biological evaluations of 1, 2, 3- triazolyl-tethered 4-quinolone ferrocene conjugates

1, 2, 3-Triazoles have attracted considerable attention in recent years because of their wide range of biological activities against various viruses, malignant cells, microorganisms and their inhibitory activities against several enzymes [1]. Advances in the rational design of metalbased therapeutic agents have increased after the discovery of cisplatin, which has been the main impetus for the expansion of metal complexes in cancer and other pathologies. The introduction of a ferrocenyl (Fc) moiety into a drug molecule has now been recognized as a useful approach for the development of more effective therapeutic applications [2].Novel 4-quinolone-ferrocene conjugates linked via 1, 2, 3-triazolyl scaffold were synthesized by regioselective Cu(I)- catalyzed 1, 3-dipolar cycloaddition of corresponding azide and alkynyl derivatives. Azido intermediates were synthesyzed from hydroxyl or bromoethyl analogs, while alkynyl derivatives of quinolones were prepared by alkylation in the presence of base. Although N-alkylation process of the quinolone system is both thermodynamically and kinetically favored, the introduction of trifluoromethyl group at C2-position makes this reaction kinetically less favored. Results of biological evaluat ions for newly synthesized compounds will be presented.

1, 2, 3-triazole, quinolone, ferrocene

nije evidentirano