title: Antiproliferative Activity of Polyether Antibiotic--Cinchona Alkaloid Conjugates Obtained via Click Chemistry.
abstract: A series of eight new conjugates of salinomycin or monensin and Cinchona alkaloids were obtained by the Cu(I)-catalysed 1,3-dipolar Huisgen cycloaddition (click chemistry) of respective N-propargyl amides of salinomycin or monensin with four different Cinchona alkaloid derived azides. In vitro antiproliferative activity of these conjugates evaluated against three cancer cell lines (LoVo, LoVo/DX, HepG2) showed that four of the compounds exhibited high antiproliferative activity (IC50 below 3.00 μm) and appeared to be less toxic and more selective against normal cells than two standard anticancer drugs.
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614, Poznan, Poland.
authors.forename: Iwona
authors.initials: I
authors.lastname: Skiera
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614, Poznan, Poland.
authors.forename: Michał
authors.initials: M
authors.lastname: Antoszczak
authors.affiliation: Ludwik Hierszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Rudolfa Weigla 12, 53-114, Wroclaw, Poland.
authors.forename: Justyna
authors.initials: J
authors.lastname: Trynda
authors.affiliation: Ludwik Hierszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Rudolfa Weigla 12, 53-114, Wroclaw, Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Wietrzyk
authors.affiliation: Faculty of Chemistry, Wrocław University of Technology, Wyspiańskiego 27, 50-370, Wroclaw, Poland.
authors.forename: Przemysław
authors.initials: P
authors.lastname: Boratyński
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614, Poznan, Poland.
authors.forename: Karol
authors.initials: K
authors.lastname: Kacprzak
authors.affiliation: Faculty of Chemistry, Adam Mickiewicz University, Umultowska 89b, 61-614, Poznan, Poland.
authors.forename: Adam
authors.initials: A
authors.lastname: Huczyński
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002930:Cinchona Alkaloids / Q000737:chemistry* / Q000494:pharmacology*; D057930:Click Chemistry; D006801:Humans; D008985:Monensin / Q000737:chemistry / Q000494:pharmacology; D009369:Neoplasms / Q000188:drug therapy; D011714:Pyrans / Q000737:chemistry / Q000494:pharmacology; D000095662:Polyether Polyketides
chemical_list: D000900:Anti-Bacterial Agents; D000970:Antineoplastic Agents; D002930:Cinchona Alkaloids; D008985:Monensin; D011714:Pyrans; C010327:salinomycin; D000095662:Polyether Polyketides
keywords: Cinchona alkaloids; anticancer activity; click chemistry; monensin; salinomycin