title: Synthesis and biological activity of diisothiocyanate-derived mercapturic acids.
abstract: This Letter deals with new non-natural diisothiocyanates, their mercapturic acid derivatives-conjugated with N-acetylcysteine as well as their antiproliferative activity towards human colon cancer cell lines and their inhibitory potency towards histone deacetylase activity. The activity of analysed isothiocyanates is not significantly different than their N-acetylcysteine conjugates. In comparison to simple mono-isothiocyanate analogues, aliphatic diisothiocyanates and their conjugates are much more active than the simple presence of two isothiocyanate functionalities could indicate.
authors.affiliation: Division of Medicinal Chemistry and Microbiology, Faculty of Chemistry, Wrocław University of Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.
authors.forename: Renata
authors.initials: R
authors.lastname: Grzywa
authors.affiliation: Division of Medicinal Chemistry and Microbiology, Faculty of Chemistry, Wrocław University of Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.
authors.forename: Łukasz
authors.initials: Ł
authors.lastname: Winiarski
authors.affiliation: Division of Medicinal Chemistry and Microbiology, Faculty of Chemistry, Wrocław University of Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland; Department of Experimental Oncology, Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, R. Weigla St. 12, Wrocław 53-114, Poland.
authors.forename: Mateusz
authors.initials: M
authors.lastname: Psurski
authors.affiliation: Division of Medicinal Chemistry and Microbiology, Faculty of Chemistry, Wrocław University of Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.
authors.forename: Agata
authors.initials: A
authors.lastname: Rudnicka
authors.affiliation: Department of Experimental Oncology, Ludwik Hirszfeld Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, R. Weigla St. 12, Wrocław 53-114, Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Wietrzyk
authors.affiliation: Institute of Organic Chemistry, Faculty of Chemistry, Technical University of Lodz, Żeromskiego St. 116, 90-924 Łódź, Poland.
authors.forename: Tadeusz
authors.initials: T
authors.lastname: Gajda
authors.affiliation: Division of Medicinal Chemistry and Microbiology, Faculty of Chemistry, Wrocław University of Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland. Electronic address: jozef.oleksyszyn@pwr.edu.pl.
authors.forename: Józef
authors.initials: J
authors.lastname: Oleksyszyn
mesh_terms: D000111:Acetylcysteine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D003106:Colon / Q000187:drug effects / Q000473:pathology; D003110:Colonic Neoplasms / Q000188:drug therapy / Q000473:pathology; D006801:Humans; D017879:Isothiocyanates / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D017879:Isothiocyanates; D000111:Acetylcysteine
keywords: Colon cancer cell line; Diisothiocyanate; Histone deacetylase; Mercapturic acid