Design, Synthesis, and Anti-Proliferative Activity of Quinoxaline Linked 1,2,4-Oxadiazole Hybrids

Herein, synthesis of some new quinoxaline-1,2,4-oxadiazole derivatives is presented, and their in vitro anti-cancer activity against four human cancer cell lines like MCF-7 (human breast), HeLa (human cervical), HCT116 (human colon carcinoma) HepG2 (liver hepato cellular carcinoma) is tested. The results reveal promising results for four products. One of the products displays higher activity against all tested cell lines than the standard drug etoposide. Molecular docking studies of the products on EGFR receptor suggest that the most potent compound strongly binds to protein EGFR (pdbid: 4HJO). Two compounds exhibit promising inhibitory activity of tyrosine kinase EGFR.

Automated summary

This study presents the synthesis of new quinoxaline-1,2,4-oxadiazole derivatives and examines their in vitro anti-cancer activity against four human cancer cell lines. The results reveal promising anti-cancer activity for four of the tested products, with one product showing higher activity than the standard drug etoposide against all tested cell lines. Molecular docking studies suggest that the most potent compound strongly binds to the EGFR protein. Two compounds also exhibit promising inhibitory activity of the tyrosine kinase EGFR.