Synthesis of some benzylidene thiosemicarbazide derivatives and evaluation of their cytotoxicity on U87, MCF-7, A549, 3T3 and HUVEC cell lines

Abstract

Iron homeostasis is altered in tumours in response to a perturbation in the expression of iron-dependent proteins. Therefore, iron chelators make cancerous cells more vulnerable to iron deficiency. Compounds having thiosemicarbazide scaffold with the ability to metal complex formation have the potential to act as anticancer. A series of thiosemicarbazide derivatives were designed, synthesized successfully and their cytotoxicity was then tested on some cancerous as well as laboratory normal model systems by using colorimetric assay based on WST-1 reagent. According to the cytotoxicity results, some compounds showed high toxicity effect on both the cancerous and healthy cell lines. The results of toxicity assays on U87 and A549 cell lines showed the survivability less than 50 % at all concentrations higher than 10 ppm for all the synthesized compounds. The MCF-7 cell line exhibited approximately the same behaviour and had survivability less than 60 %. The 3T3 in compared with HUVEC cell line showed a completely different behaviour against the synthesized compounds and had survivability more than 50 %. The selectivity index was also measured and based on the study results it could be concluded that the cytotoxicity profile of the synthesized compounds on 3T3 cell line shows a significant difference, indicating a good anticancer effect of these compounds.

Keywords

• meta and para-substituted benzyliden thiosemicasrbazides
• cyto-toxicity assessment
• cancerous and normal cell lines
• wst-1 assay