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Design, Synthesis and Molecular Docking of Novel Quinazolinone Hydrazide Derivatives as EGFR Inhibitors by Ze‐Yu Fang; Yi‐Heng Zhang; Chong‐Hao Chen; Qi Zheng; Peng‐Cheng Lv; Lei‐Qiang Ni; Juan Sun; Yuan‐Feng Wu is a Agricultural and Biological Sciences article available to read on EtoBox.
What is Design, Synthesis and Molecular Docking of Novel Quinazolinone Hydrazide Derivatives as EGFR Inhibitors about?
## Abstract A series of novel quinazolinone hydrazide derivatives were designed and synthesized as EGFR inhibitors. The results indicated that most of the aimed compounds had potential anti‐tumor cell proliferation and EGFR inhibitory activities. In the comprehensive analysis of all the tested compounds, the target compound 9c showed the best anti‐tumor cell proliferation activity, (IC~50~=1.31 μM for MCF‐7, IC~50~=1.89 μM for HepG2, IC~50~=2.10 μM for SGC), and IC~50~=0.59 μM for the EGFR inhibitory activity. Docking results showed that compound 9c could ideally insert the active site and interact with the critical amino acid residues (Val702, Lys721, Met769, Asp831) in the active site.
Who reads Design, Synthesis and Molecular Docking of Novel Quinazolinone Hydrazide Derivatives as EGFR Inhibitors?
It is typically read by researchers, students, and practitioners in Agricultural and Biological Sciences.
- Author
- Ze‐Yu Fang; Yi‐Heng Zhang; Chong‐Hao Chen; Qi Zheng; Peng‐Cheng Lv; Lei‐Qiang Ni; Juan Sun; Yuan‐Feng Wu
- Publisher
- Wiley
- Published
- 2022
- Language
- EN
- Field
- Agricultural and Biological Sciences (Life Sciences)