DESIGN, SYNTHESIS, AND EVALUATION OF 1,4-NAPHTHOQUINONE DERIVATIVES AS POTENTIAL EPITHELIAL GROWTH FACTOR RECEPTOR INHIBITORSAbstract
In this manuscript, we designed and synthesized 1,4-naphthoquinone derivatives. These derivatives were characterized using the different analytical techniques such as 1H NMR, 13C NMR, FTIR, Mass spectroscopy, melting point, and elemental analysis. The synthesized compounds (MB (1-10)) further subjected to assess the anticancer activity using different cancer cell lines such as MCF-7, HeLa, and HepG2. The compound MB-10 was observed to be the most active against these three cancer cell lines i.e. MCF-7 (IC50 = 16.13± 0.29 µM), HeLa (IC50 = 12.98 ± 0.37 µM) and HepG2 (IC50 = 18.73 ± 0.65 µM). Compound MB10 has also shown potent tyrosine kinase inhibitory activity with IC50 = 1.23 ± 0.12 µM. Moreover, molecular docking investigation revealed that compound MB-10 has strong binding affinity to the amino residue of the active site of enzyme protein tyrosine kinase, which contingent the cytotoxic activities. These outcomes give promising beginning stages to assist in the improvement of cancer as novel and powerful anticancer agents.
M. Besan *, M. K. Gautam and A. Jain
Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, Uttar Pradesh, India.
12 March 2019
10 May 2019
30 May 2019
01 December 2019