1Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology, (Banaras Hindu University), Varanasi-221005, India
2University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India
*For Correspondence - skshrivastava.phe@itbhu.ac.in
Online published on 30 December, 2019.
In this manuscript we have designed and synthesized 1, 4-Naphthoquinone analogs substituted with 1, 3, 4 Oxadiazolenucleus. The synthesized compound (M1-M14) were characterized using the different analytical technique1H NMR, 13C NMR, FTIR, Mass spectroscopy, melting point, elemental analysis and further subjected for the evaluation of their anticancer activity using MCF-7, Hela and HepG2 cancer cell lines. The compound M-5 was found to exhibit most potent cytotoxicity against cancer cell lines i.e. HeLa (IC50 =10.76 ± 0.11 μM), MCF7 (IC50 = 9.30 ± 0.14 μM) and HepG2 (IC50 = 11.93 ± 0.38μM). Compound M-5 has also shown potent tyrosine kinase inhibitory activity with IC50 = 1.53 ± 0.05 μM. Moreover, molecular docking has exposed that compound M-5 has strong binding affinity to the active site of tyrosine kinase. These results give promising beginning stages to assist in the improvement of novel and powerful anticancer agents.
Molecular Docking, Cytotoxicity Evaluation, 1, 3, 4 Oxadiazole, Tyrosine Kinase Inhibition
