Synthesis, structure and in vitro cytostatic activity of ferrocene-Cinchona hybrids

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:26

Article

Kocsis, Laszlo¹  Szabo, Ildiko²  Bosze, Szilvia²  Jernei, Tamas³  Hudecz, Ferenc^1,2  Csampai, Antal³ 

[1] MTA ELTE Res Grp Peptide Chem, Pazmany P Setany 1-A, H-1117 Budapest, Hungary

[2] Eotvos Lorand Univ, Dept Organ Chem, Pazmany P Setany 1-A, H-1117 Budapest, Hungary

[3] Eotvos Lorand Univ, Dept Inorgan Chem, Pazmany P Setany 1-A, H-1117 Budapest, Hungary

关键词: Ferrocene;    Cinchona;    1,2,3-Triazole;    Click reaction;    Cytostatic activity;   

DOI  :  10.1016/j.bmcl.2015.12.059

来源: Elsevier

【 摘 要 】

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 letter on the incorporation of ferrocene nucleus in the reputed cinchona family via triazole and chalcone linkers with established pharmaceutical profile. (C) 2015 Elsevier Ltd. All rights reserved.

【 授权许可】

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