title: Synthesis and antiproliferative activity of some 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles.
abstract: A series of new 5-substituted 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles has been synthesised and evaluated for their antiproliferative activity. The compounds were prepared by the reaction of the sulphinylbis(2,4-dihydroxythiobenzoyl) (STB) wit hydrazides or carbazates. The panel substitution included alkyl, alkoxy, aryl and heteroaryl derivatives. The structures of compounds were identified from the elemental, IR, (1)H NMR and MS spectra analysis. The highest antiproliferative activity against the cells of human cancer lines for 2-(2,4-dihydroxyphenyl)-5-(4-methoxybenzyloxy)-1,3,4-thiadiazole was found with ID(50) values comparable (HCV29T and SW707) or significantly lower (T47D) than for cisplatin applied as the reference compound. The influence of 5-substiution type of 2-(2,4-dihydroxyphenyl)-1,3,4-thiadiazoles on antiproliferative activity is discussed.
authors.affiliation: Department of Chemistry, Agricultural University, Lublin, Poland. joanna.matysiak@ar.lublin.pl
authors.forename: Joanna
authors.initials: J
authors.lastname: Matysiak
authors.forename: Anna
authors.initials: A
authors.lastname: Nasulewicz
authors.forename: Marzena
authors.initials: M
authors.lastname: Pełczyńska
authors.forename: Marta
authors.initials: M
authors.lastname: Switalska
authors.forename: Iwona
authors.initials: I
authors.lastname: Jaroszewicz
authors.forename: Adam
authors.initials: A
authors.lastname: Opolski
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002945:Cisplatin / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006860:Hydrogen Bonding; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D011955:Receptors, Drug / Q000737:chemistry / Q000187:drug effects; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D001749:Urinary Bladder Neoplasms / Q000188:drug therapy / Q000473:pathology
chemical_list: D000970:Antineoplastic Agents; D007202:Indicators and Reagents; D011955:Receptors, Drug; D013830:Thiadiazoles; D002945:Cisplatin