EGFR kinase inhibitors from novel thiazole derivatives: synthesis, anticolon cancer, docking, and ADME studies.

Authors

Amani M R Alsaedi, Alaa M Abu Alnjaa, Amel S Younes, Zeinab A Muhammad, Sami A Al-Hussain, Magdi E A Zaki, Thoraya A Farghaly

Published in

Future medicinal chemistry. Pages 1-11. Sep 01, 2026. Epub Sep 01, 2026.

Abstract

The epidermal growth factor receptor (EGFR) is a key regulator of malignant cell growth and survival, making it an attractive target for cancer therapy. In this study, a new series of thiazole derivatives was rationally designed and synthesized as potential EGFR inhibitors and evaluated for their antiproliferative activity against two human colon cancer cell lines (HCT-116 and HT29). Several compounds exhibited potent anticancer activity, with compound 4j showing the highest potency, displaying half-maximal inhibitory concentration (IC₅₀) values of 2.10 and 1.91 µM against HCT-116 and HT29 cells, respectively. Owing to its superior antiproliferative activity, compound 4j was further evaluated for EGFR inhibitory activity and demonstrated remarkable potency with an IC₅₀ value of 0.27 µM. In addition, 4j exhibited a favorable selectivity index toward normal WI38 cells and effectively induced apoptosis through modulation of Bax, Bcl-2, and p53 expression. Molecular docking demonstrated strong binding interactions of 4j within the EGFR active site, while its ADME predictions supported its favorable drug-like profile. Overall, compound 4j represents a promising lead candidate for the development of novel EGFR-targeted anticancer agents.

PMID:
42678354
Bibliographic data and abstract were imported from PubMed on 01 Sep 2026.

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