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Letters in Drug Design & Discovery

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ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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Research Article

Synthesis and Biological Evaluation of 3,9-Dioxatetraasteranes as Potential Inhibitors of Epidermal Growth Factor Receptor

Author(s): Hongjun Wang, Nana Tian, Dongchen Chu and Hong Yan*

Volume 21, Issue 3, 2024

Published on: 27 October, 2022

Page: [552 - 558] Pages: 7

DOI: 10.2174/1570180819666220928151144

Price: $65

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.

Keywords: EGFR inhibitors, 3, 9-dioxatetraasteranes, antiproliferative activity, molecular docking, A549 and HepG2 cell lines

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