Synthesis and Biological Evaluation of New Pyrazole-based Thiazolyl Hydrazone Derivatives as Potential Anticancer Agents

Title:Synthesis and Biological Evaluation of New Pyrazole-based Thiazolyl Hydrazone Derivatives as Potential Anticancer Agents

Volume: 11 Issue: 7

Author(s): Mehlika Dilek Altıntop, Ahmet Ozdemir, Sinem Ilgın and Ozlem Atli

Affiliation:

Keywords: Anticancer activity, Hydrazone, Pyrazole, Thiazole.

Abstract: New pyrazole-based thiazolyl hydrazone derivatives were obtained via the ring closure reaction of 3,5- dimethyl-1H-1-phenylpyrazole-4-carboxaldehyde thiosemicarbazone with 2-bromoacetophenone derivatives. The compounds were investigated for their cytotoxic effects on A549 and NIH3T3 cell lines. Among these compounds, compound 2i bearing a trifluoromethyl substituent can be identified as the most promising anticancer agent against A549 cancer cell lines. Compound 2i exhibited its inhibitory effect on A549 cells with an IC₅₀ value of 0.0316 mM, whereas cisplatin showed its anticancer activity with an IC₅₀ value of 0.01 mM. According to the IC₅₀ values, the inhibitory effect of compound 2i on A549 cells can be considered to be selective when compared with its effect on NIH3T3 cells.

Cite this article as:

Altıntop Dilek Mehlika, Ozdemir Ahmet, Ilgın Sinem and Atli Ozlem, Synthesis and Biological Evaluation of New Pyrazole-based Thiazolyl Hydrazone Derivatives as Potential Anticancer Agents, Letters in Drug Design & Discovery 2014; 11(7) . https://dx.doi.org/10.2174/1570180811666140226235350