Development of 1, 4-naphthoquinones as potential epidermal growth factor receptor inhibitors for the treatment of cancer

Abstract

In this manuscript, we have designed, synthesized and characterized 1, 4-naphthoquinone derivatives. The synthesized compounds (MB1-MB19) were further subjected for evaluation of their anticancer activity using MCF-7, 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. © 2019, Association of Biotechnology and Pharmacy. All rights reserved.