A series of new pyrazole/quinoline hybrids 11a-n was constructed and synthesized as prospective antiproliferative agents. The antiproliferative activities of the newly synthesized hybrids were assessed against a panel of four human cancer cells: HT-29, A-549, Panc-1, and MCF-7. Hybrids 11c, 11d, 11h, 11i, and 11k demonstrated remarkable antiproliferative activity, with IC ranging from 36 to 61 nM, compared to erlotinib, which had IC ranging from 30 to 40 nM. Hybrid 11i was the most potent EGFR inhibitor with an IC of 87 nM and exhibited comparable EGFR inhibition to that of erlotinib (IC = 80 nM). Molecular docking study results in the EGFR active site agreed with the EGFR inhibitory activity results.
Keywords: EGFR, anti‐proliferative, hydrazone, pyrazole, quinoline
Chemical biology & drug design
Journal Article
English
41637654
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