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

Russian Journal of General Chemistry(2022)

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Abstract
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.
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Key words
quinoxaline-1, 2, 4-oxadiazole, in vitro anticancer activity, molecular docking studies, in vitro tyrosine kinase EGFR inhibitory activity, SAR studies
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