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Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors
- Publication Year :
- 2022
- Publisher :
- Taylor & Francis, 2022.
-
Abstract
- This paper described our efforts to develop dianilinopyrimidines as novel EGFR inhibitors. All the target compounds were tested for inhibitory effects against wild type EGFR (EGFRwt) and three tumour cells, including A549, PC-3, and HepG2. Some of the compounds performed well in antitumor activities. Especially, compound 4c 2-((2-((4-(3-fluorobenzamido)phenyl)amino)-5-(trifluoromethyl) pyrimidin-4-yl)amino)-N-methylthiophene-3-carboxamide showed higher anti-tumour activities than Gefitinib. The IC50 values of compound 4c against A549, PC-3, and HepG2. reached 0.56 μM, 2.46 μM, and 2.21 μM, respectively. In addition, further studies indicated that compound 4c could induce apoptosis against A549 cells and arrest A549 cells in the G2/M phase. Molecular docking studies showed that compound 4c could closely interact with EGFR. Generally, compound 4c was the potential for developing into an anti-tumour drug.
- Subjects :
- Pharmacology
Aniline Compounds
Dose-Response Relationship, Drug
Molecular Structure
Cell Cycle
Antineoplastic Agents
Apoptosis
General Medicine
ErbB Receptors
Molecular Docking Simulation
Structure-Activity Relationship
Pyrimidines
Cell Line, Tumor
Drug Design
Drug Discovery
Humans
Drug Screening Assays, Antitumor
Protein Kinase Inhibitors
Cell Proliferation
Subjects
Details
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....3376c31285035504bf578fde82f1a9f0
- Full Text :
- https://doi.org/10.6084/m9.figshare.19328841