title: Synthesis, structure and in vitro cytostatic activity of ferrocene-Cinchona hybrids.
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 letter on the incorporation of ferrocene nucleus in the reputed cinchona family via triazole and chalcone linkers with established pharmaceutical profile.
authors.affiliation: MTA-ELTE Research Group of Peptide Chemistry, Budapest Pázmány P. sétány 1/A, H-1117, Hungary.
authors.forename: László
authors.initials: L
authors.lastname: Kocsis
authors.affiliation: Department of Organic Chemistry, Eötvös Loránd University (ELTE), Budapest Pázmány P. sétány 1/A, H-1117, Hungary.
authors.forename: Ildikó
authors.initials: I
authors.lastname: Szabó
authors.affiliation: Department of Organic Chemistry, Eötvös Loránd University (ELTE), Budapest Pázmány P. sétány 1/A, H-1117, Hungary.
authors.forename: Szilvia
authors.initials: S
authors.lastname: Bősze
authors.affiliation: Department of Inorganic Chemistry, Eötvös Loránd University (ELTE), Budapest Pázmány P. sétány 1/A, H-1117, Hungary.
authors.forename: Tamás
authors.initials: T
authors.lastname: Jernei
authors.affiliation: MTA-ELTE Research Group of Peptide Chemistry, Budapest Pázmány P. sétány 1/A, H-1117, Hungary; Department of Organic Chemistry, Eötvös Loránd University (ELTE), Budapest Pázmány P. sétány 1/A, H-1117, Hungary.
authors.forename: Ferenc
authors.initials: F
authors.lastname: Hudecz
authors.affiliation: Department of Inorganic Chemistry, Eötvös Loránd University (ELTE), Budapest Pázmány P. sétány 1/A, H-1117, Hungary. Electronic address: csampai@chem.elte.hu.
authors.forename: Antal
authors.initials: A
authors.lastname: Csámpai
mesh_terms: D000480:Alkynes / Q000737:chemistry; D001386:Azides / Q000737:chemistry; D002384:Catalysis; D049109:Cell Proliferation / Q000187:drug effects; D002929:Cinchona / Q000737:chemistry*; D003300:Copper / Q000737:chemistry; D061565:Cycloaddition Reaction; D054697:Cytostatic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005296:Ferrous Compounds / Q000737:chemistry*; D019073:HT29 Cells; D056945:Hep G2 Cells; D006801:Humans; D000075163:Metallocenes; D012428:Ruthenium / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000480:Alkynes; D001386:Azides; D054697:Cytostatic Agents; D005296:Ferrous Compounds; D000075163:Metallocenes; D003300:Copper; D012428:Ruthenium; C004998:ferrocene
keywords: 1,2,3-Triazole; Cinchona; Click reaction; Cytostatic activity; Ferrocene