Synthesis, structural elucidation and cytotoxicity of new thiosemicarbazone derivatives

Abstract

Syntheses and characterization (1H & 13C NMR and CHN) of four new thiosemicarbazone derivatives (1–4) are reported. The molecular structures of compounds 1–4 were determined using single crystal X-ray crystallographic technique. Cytotoxic effect of all the compounds was determined against three cancerous (PANC-1, HCT 116 and MCF-7) and one non-cancerous (NIH/3T3) cell lines. All the compounds remained safe against non-cancerous cells (IC50 > 500 μM) but induced significant cytotoxicity in the cancerous cell lines. Importantly, compounds 2 and 4 showed excellent cytotoxicity (IC50 = 10.0 and 0.7 μM against PANC-1; 14.9 and 9.4 μM against HCT 116; 14.3 and 15.8 μM against MCF-7 for 2 and 4 respectively). Based on the results it can be concluded that the thiosemicarbazone derivatives (2 and 4) can be further studied in detail for the purpose of chemotherapeutic drug development. Keywords: Thiosemicarbazones, Crystal structures, Antitumor agents, Bioorganic chemistry, Cytotoxicity