Design, synthesis and antitumor activity of new naproxen based 1,2,4-triazole-Schiff base derivatives

Abstract

In the present work, new Naproxen based 1,2,4-triazole-Schiff base derivatives have been synthesized and screened for in vitro antitumor activity and in silico pharmacokinetic studies. The structure of the newly synthesized compounds (5–12) was elucidated by IR, NMR and mass spectrometry. All the compounds were tested against breast MCF-7, hepatocellular Huh-7 and lung A-549 cancer cell lines using MTT assay. Compound 7 was better in killing A549 cells with IC50 3.71 µM (1.48 fold), compared with Doxorubicin (IC50 5.50 µM). Also, compound 7 was found to be non toxic on MRC-5 normal cells as it depicts IC50 more than 500 μM. Besides, compound 12 also revealed promising activity with IC50 6.94 and 3.33 µM against MCF-7 and Huh-7 respectively. The in silico studies displayed that the synthesized compounds favors the desired pharmacokinetic profile and drug likeness properties. It can be concluded that these new Naproxen based 1,2,4-triazole-Schiff base derivative (7) has the potential to be further investigated as lead molecule in the development of new chemotherapeutic agent.