Benzoxazole-appended piperidine derivatives as novel anticancer candidates against breast cancer

Bioorganic Chemistry(2023)

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摘要
•New benzoxazole-appended piperidine derivatives were designed, synthesized as promising anti-breast cancer candidates.•Thirty compounds were screened by MTT assay and many of them were potent antiproliferative agents towards MCF-7 and/or MDA-MB-231 cells.•Compounds 4d, 7h and 12g were notable EGFR inhibitors while all tested compounds displayed less ARO inhibition activity than letrozole.•Tested compounds showed promising caspase-9 activation and cell cycle arrest mainly at the S phase.•Docking studies revealed activity aganist EGFR similar to erlotinib.
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关键词
Benzoxazole-appended piperidines, 1,2,4-triazole-5-thiones,Anti-breast cancer activity,Enzymes inhibition,Apoptosis,Docking study
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