Synthesis of N-substituted- N-acylthioureas of 4-substituted piperazines endowed with local anaesthetic, antihyperlipidemic, antiproliferative activities and antiarrythmic, analgesic, antiaggregating actions (original) (raw)
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Medicinal Chemistry Research
The reaction of 2-isonicotinoyl-N-cyclohexyl/ arylhydrazinecarbothioamide (2a–r) with sodium hydroxide, in each case, a single product was obtained. The structures of the compounds were confirmed on the basis of their elemental analysis and spectral data. The single crystal X-ray analysis confirmed the structure of these products as N-4-cyclohexyl/aryl-5-(pyridine-4-yl)-2,4- dihydro-3H-1,2,4-triazole-3-thiones (3a–r). The in vitro antitumor activity of compounds was screened against three cell lines; BEL-7402, HUH-7 and HepG2 human hepatoma using MTT assay. Sorafenib (50 lM) was used as a positive control. The results of the MTT-dye reduction assay indicated that most of the compounds exert potent cytotoxic/antiproliferative effect in a time and dosedependent manner via induced apoptosis of HepG2 cells.