Synthesis, cytotoxic evaluation of substituted cinnamic-based 1,2,4-triazolo thiadiazoles

Abstract

In an attempt to find a new class of cytotoxic agents, a series of 3,6-disubstituted-[1,2,4] triazolo[3,4-<em>b</em>] [1,3,4]thiadiazoles have been synthesized using undecenoic acid and various cinnamic acids. The structures of the synthesized compounds have been confirmed using ¹H and ¹³C NMR, IR and mass spectroscopy. The prepared compounds have been evaluated for their <em>in vitro</em> cytotoxic activities against four human cancer cell lines namely, HeLa, B16-F10, SKOV3, MCF7 and CHO-K1 Normal Cell line using MTT assay. Compounds <strong>6a</strong> and <strong>6h </strong>show promising activity against HeLa (IC₅₀ value 8.92µM) and SKOV3 cell lines (IC₅₀ value 9.43 µM). Majority of the compounds show significant activities against HeLa cell line with the IC₅₀ values ranging from 8.92 to 13.44 μM. All the compounds show good activity against SKOV3 cell line with the IC₅₀ values ranging from 9.43 to 19.34 μM. Majority of the compounds are non toxic towards the Chinese hamster ovary (CHO-K1) normal cell line.