DOI: 10.4155/fmc-2023-0086 ISSN: 1756-8919

Discovery of new thieno[2,3-d]pyrimidines as EGFR tyrosine kinase inhibitors for cancer treatment

Eman A Sobh, Mohammed A Dahab, Eslam B Elkaeed, Aisha A Alsfouk, Ibrahim M Ibrahim, Ahmed M Metwaly, Ibrahim H Eissa
  • Drug Discovery
  • Pharmacology
  • Molecular Medicine

Background: EGFR has been considered a vital molecular target in cancer management. Aim: The discovery of new thieno[2,3- d]pyrimidine derivatives as EGFR tyrosine kinase inhibitors. Methods: Nine derivatives were designed, synthesized and subjected to in vitro and in silico studies. Results: Compound 7a significantly inhibited the growth of HepG2 and PC3 cells for both EGFR wild-type and EGFRT790M. Compound 7a caused a significant apoptotic effect, arresting HepG2 cells’ growth in the S and G2/M phases. Docking and molecular dynamics simulation studies confirmed the correct and stable binding modes of the synthesized compounds against the active sites. Conclusion: Compound 7a is a promising dual EGFR inhibitor for cancer treatment.

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