Synthesis and antitumor activity of 4-cyclohexyl/aryl-5-(pyridin-4-yl)-2, 4-dihydro-3H-1, 2, 4-triazole-3-thiones.

Journal Article

Fun, Mashooq Ahmad Bhat, Mohamed A Al-Omar, Ahmed M Naglah, Mohamed M Abdulla, Hoong-Kun . 2015

• Magazine \ Newspaper: Med. Chem. Res.
• Volume Number: 24
• Pages: 1558-1567

Publication Abstract

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.