A series of 3,6-disubstituted 1,2,4–triazolo[3,4-b]-1,3,4-thiadiazoles were synthesized from 3- substituted-4-amino-5-mercapto-1,2,4-triazoles and 3-substituted 4-carboxypyrazoles. Elemental analyses, IR, 1H NMR and mass spectral data confirmed the structures of all newly synthesized compounds. Most of the newly synthesized compounds were screened for their anticancer activity in hepatic cell lines. Many of the compounds were found to be potent. The perturbations brought by the substituent can affect various parameters of the molecule like its electron density, its steric environment, its bioavailability etc. The thiadiazole with naphthyloxymethyl and fluorophenyl groups as substituents showed excellent antiproliferative effect
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