Synthesis, structural elucidation and cytotoxicity of new thiosemicarbazone derivatives

Syntheses and characterization (H-1 & C-13 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 - mu M) but induced significant cytotoxicity in the cancerous cell lines. Importantly, compounds 2 and 4 showed excellent cytotoxicity (IC50 = 10.0 and 0.7 mu M against PANC-1; 14.9 and 9.4 mu M against HCT 116; 14.3 and 15.8 mu M 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. (C) 2015 The Authors. Published by Elsevier B.V. on behalf of King Saud University.