Development of 1, 4-Naphthoquinones as Potential Epidermal Growth Factor Receptor Inhibitors For The Treatment of Cancer Besan Mousumi1, Gautam Manoj K.2, Shrivastava Sushant K.1,* 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@iitbhu.ac.in
Online published on 30 December, 2019. Abstract In this manuscript, we have designed, synthesized and characterized 1, 4naphthoquinone derivatives. The synthesized compounds (MB1-MB19) were further subjected for evaluation of their anticancer activity using MCF7, HeLa and HepG2 cancer cell lines. The compound MB-9 was observed to be most active against these three cancer cell lines i.e. MCF-7 (IC50= 15.63 ±0.47 μM), HeLa (IC50=13.45 ± 0.48 μM), and HepG2 (IC50 = 23.87 ± 0.59μM). Compound MB-9 has also shown potent tyrosine kinase inhibitory activity with IC50 = 1.80 ± 0.06 μM. Moreover, molecular docking investigations revealed that compound MB-9 has strong binding affinity to the active site residues of tyrosine kinase. These outcomes give a promising beginning to assist in the improvement of novel and powerful anticancer agents. Top Keywords Molecular Docking, In-vitro cytotoxicity, 1, 4-Naphthoquinone, Tyrosine kinase, Epidermal growth factor receptor. Top |