title: A review on acridinylthioureas and its derivatives: biological and cytotoxic activity.
abstract: Acridines possess two characteristics that have led many researchers to consider the agents interesting targets for future development as potential farmacophores: the planar acridine skeleton, which is able to intercalate into DNA, and the intense fluorescence of the agents. This review offers a study of the multifunctional character of acridines and the synthesis of novel acridine derivatives, with particular focus being placed on isothiocyanates and their congeners, e.g. thioureas, isothioureas, quaternary ammonium salts and platinum/gold conjugates. The review provides an overview of the structure, spectral properties, DNA binding and biological activity of acridinylthiourea congeners. These acridinylthiourea derivatives display significant cytotoxic activities against different types of cancer cell lines at micromolar concentrations. Copyright © 2017 John Wiley & Sons, Ltd.
authors.affiliation: Department of Biochemisty, Institute of Chemistry, P.J. Šafárik University Košice, Moyzesova 11, Košice, Slovak Republic.|Biomedical Research Center, University Hospital Hradec Kralove, Sokolovska 581, Hradec Kralove, Czech Republic.
authors.forename: Mária
authors.identifier: http://orcid.org/0000-0002-2789-8397
authors.initials: M
authors.lastname: Kožurková
authors.affiliation: Department of Biochemisty, Institute of Chemistry, P.J. Šafárik University Košice, Moyzesova 11, Košice, Slovak Republic.
authors.forename: Danica
authors.initials: D
authors.lastname: Sabolová
authors.affiliation: Department of Organic Chemistry, Institute of Chemistry, P.J. Šafárik University Košice, Moyzesova 11, Košice, Slovak Republic.
authors.forename: Pavol
authors.initials: P
authors.lastname: Kristian
mesh_terms: D000166:Acridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D004249:DNA Damage / Q000187:drug effects*; D006801:Humans; D017879:Isothiocyanates / Q000138:chemical synthesis / Q000494:pharmacology; D011370:Proflavine / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013890:Thiourea / Q000138:chemical synthesis / Q000494:pharmacology
chemical_list: D000166:Acridines; D000970:Antineoplastic Agents; D017879:Isothiocyanates; D011370:Proflavine; D013890:Thiourea
keywords: Acridine; cytotoxicity; fluorescence; intercalation; isothiocyanate; platinum thioureas; synthesis; thiourea; urea