Design, synthesis and antiproliferative, apoptotic, and immunomodulatory properties of new heteroaryl pyridine-linked 1,2,4-oxadiazoles as prospective dual EGFR/BRAF V600E inhibitors
Key Points
The study aims to investigate the design and properties of novel compounds that inhibit EGFR and mutant BRAF.
Synthesis of heteroaryl pyridine-linked 1,2,4-oxadiazoles
Evaluation of antiproliferative effects in vitro
Assessment of apoptotic and immunomodulatory properties
Compound 21c exhibits significant inhibition of EGFR and BRAF activities.
Demonstrated enhanced antiproliferative effects compared to existing treatments.
Identified potential for improved cancer treatment through vertical blockade strategy.
Abstract
Vemurafenib triggers resistance via EGFR feedback upregulation, compound 21c achieves a “vertical blockade” by simultaneously inhibiting EGFR and mutant BRAF.
Design, synthesis and antiproliferative, apoptotic, and immunomodulatory properties of new heteroaryl pyridine-linked 1,2,4-oxadiazoles as prospective dual EGFR/BRAF V600E inhibitors | Synapse