title: Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
abstract: Iron chelators have emerged as a potential anti-cancer treatment strategy. In this study, a series of novel thiosemicarbazone iron chelators containing a quinoline scaffold were synthesized and characterized. A number of analogs show markedly greater anti-cancer activity than the 'gold-standard' iron chelator, desferrioxamine. The anti-proliferative activity and iron chelation efficacy of several of these ligands (especially compound 1b), indicates that further investigation of this class of thiosemicarbazones is worthwhile.
authors.affiliation: Department of Organic Chemistry, Institute of Chemistry, University of Silesia, PL-40006 Katowice, Poland.
authors.forename: Maciej
authors.initials: M
authors.lastname: Serda
authors.forename: Danuta S
authors.initials: DS
authors.lastname: Kalinowski
authors.forename: Anna
authors.initials: A
authors.lastname: Mrozek-Wilczkiewicz
authors.forename: Robert
authors.initials: R
authors.lastname: Musiol
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Szurko
authors.forename: Alicja
authors.initials: A
authors.lastname: Ratuszna
authors.forename: Namfon
authors.initials: N
authors.lastname: Pantarat
authors.forename: Zaklina
authors.initials: Z
authors.lastname: Kovacevic
authors.forename: Angelica M
authors.initials: AM
authors.lastname: Merlot
authors.forename: Des R
authors.initials: DR
authors.lastname: Richardson
authors.forename: Jaroslaw
authors.initials: J
authors.lastname: Polanski
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003676:Deferoxamine / Q000494:pharmacology; D006801:Humans; D007501:Iron / Q000378:metabolism; D007502:Iron Chelating Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D009369:Neoplasms / Q000188:drug therapy / Q000378:metabolism; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013882:Thiosemicarbazones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D007502:Iron Chelating Agents; D011804:Quinolines; D013882:Thiosemicarbazones; D007501:Iron; D003676:Deferoxamine