Synthesis, Structure and in vitro Cytostatic Activity of Ferrocene - Cinchona Hybrids

Kocsis, László and Szabó, Ildikó and Bősze, Szilvia and Jernei, Tamás and Hudecz, Ferenc and Csámpai, Antal (2016) Synthesis, Structure and in vitro Cytostatic Activity of Ferrocene - Cinchona Hybrids. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 26. pp. 946-949. ISSN 0960-894X

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Abstract

Exploring copper(I)- and ruthenium(II)-catalyzed azide-alkyne cycloadditions and a Sonogashira protocol, novel cytostatic ferrocene-cinchona hybrids were synthetized displaying significant in vitro activity on HEPG-2 and HT-29 cells. Preliminary SAR studies disclosed that compounds incorporating linkers with 1,2,3-triazole and chalchone residues can be considered as promising lead structures. According to the best of our knowledge this is the first report on the incorporation of ferrocene nucleus in the reputed cinchona family via triazole and chalcone linkers with established pharmaceutical profile.

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