Title:Synthesis and Biological Evaluation of 3,9-Dioxatetraasteranes as Potential
Inhibitors of Epidermal Growth Factor Receptor
Volume: 21
Issue: 3
Author(s): Hongjun Wang, Nana Tian, Dongchen Chu and Hong Yan*
Affiliation:
- Beijing Key Laboratory of Environmental and Viral Oncology, Faculty of Environment and Life, Beijing University of Technology, Beijing 100124, China
Keywords:
EGFR inhibitors, 3, 9-dioxatetraasteranes, antiproliferative activity, molecular docking, A549, HepG2 cell lines.
Abstract:
Background: Epidermal growth factor receptor (EGFR) is a validated and therapeutically
amenable target, and inhibition of the EGFR signaling pathway has emerged as an attractive target for
cancer therapy.
Methods: The present work was designed to synthesize and evaluate the antiproliferative activity of a
novel series of 3,9-dioxatetraasteranes as potential inhibitors of EGFR. All target compounds were evaluated
for antiproliferative activity in vitro against A549 and HepG2 cell lines.
Results: Among the target compounds, compound B13 displayed the most potent antiproliferative activity
against A549 with IC50 = 4.31 μM and HepG2 with IC50 = 6.92 μM. In addition, a molecular docking
study was performed to investigate the binding mode and binding capacity with EGFR (PDB code:
1M17).
Conclusion: The results indicated that 3,9-dioxatetraasteranes may be promising potential EGFR inhibitors.
