title: Synthesis and antiproliferative activity of some N'-substituted 2,4-dihydroxybenzothiohydrazides.
abstract: The paper shows that new N'-substituted 2,4-dihydroxybenzocarbothiohydrazides are able to inhibit the in vitro proliferation of human tumor cell lines. The compounds were prepared by the reaction of sulfinylbis[(2,4-dihydroxyphenyl)methanethione] (STB) or its analogs with the hydrazines. The panel of N'-substitution included aryl, pyridinyl and pyrimidinyl rings. The highest antiproliferative activity for N'-(4-(4-chlorophenyl)-6-(trifluoromethyl)pyrimidin-2-yl)-5-ethyl-2,4-dihydroxybenzothiohydrazide (5b) was found. The antiproliferative potency of some compounds was similar to that of cisplatin. Analogs with the Et substituent on benzenediol moiety displayed higher potency than with the unsubstituted one. The influence of N'-substitution on antiproliferative activity of compounds was discussed.
authors.affiliation: a Department of Chemistry , University of Life Science , Lublin , Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Matysiak
authors.affiliation: a Department of Chemistry , University of Life Science , Lublin , Poland.
authors.forename: Alicja
authors.initials: A
authors.lastname: Skrzypek
authors.affiliation: b Laboratory of Fungicide and Microbicide Technology , Institute of Industrial Organic Chemistry , Warsaw , Poland.
authors.forename: Monika
authors.initials: M
authors.lastname: Karpińska
authors.affiliation: a Department of Chemistry , University of Life Science , Lublin , Poland.
authors.forename: Urszula
authors.initials: U
authors.lastname: Głaszcz
authors.affiliation: a Department of Chemistry , University of Life Science , Lublin , Poland.|b Laboratory of Fungicide and Microbicide Technology , Institute of Industrial Organic Chemistry , Warsaw , Poland.
authors.forename: Andrzej
authors.initials: A
authors.lastname: Niewiadomy
authors.affiliation: c Department of Medicinal Chemistry , Medical University of Lublin , Lublin , Poland , and.
authors.forename: Beata
authors.initials: B
authors.lastname: Paw
authors.affiliation: a Department of Chemistry , University of Life Science , Lublin , Poland.
authors.forename: Bogusław
authors.initials: B
authors.lastname: Senczyna
authors.affiliation: d Polish Academy of Sciences, Institute of Immunology and Experimental Therapy , Wrocław , Poland.
authors.forename: Joanna
authors.initials: J
authors.lastname: Wietrzyk
authors.affiliation: d Polish Academy of Sciences, Institute of Immunology and Experimental Therapy , Wrocław , Poland.
authors.forename: Dagmara
authors.initials: D
authors.lastname: Kłopotowska
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: C000614352:2,4-dihydroxybenzocarbothiohydrazide; D000970:Antineoplastic Agents; D006834:Hydrazines
keywords: 2,4-dihydroxybenzothiohydrazide; antiproliferative activity; human cancer cell lines; synthesis