Current Trends in Biotechnology and Pharmacy

Open Access
SCOPUS
  • Year: 2019
  • Volume: 13
  • Issue: 3

Development of 1, 4-Naphthoquinones as Potential Epidermal Growth Factor Receptor Inhibitors For The Treatment of Cancer

  • Author:
  • Mousumi Besan1, Manoj K. Gautam2, Sushant K. Shrivastava1,
  • Total Page Count: 26
  • DOI:
  • Page Number: 283 to 308

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

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.

Keywords

Molecular Docking, In-vitro cytotoxicity, 1, 4-Naphthoquinone, Tyrosine kinase, Epidermal growth factor receptor