Synthesis of novel heterocyclic compounds bearing tetralin moiety of potential anticancer activity targeting the intrinsic apoptotic pathway
SYNTHETIC COMMUNICATIONS(2023)
摘要
This study deals with the readily reaction of the enaminone derivative 3 with different reagents to give the corresponding pyrazolo[3,4-b]pyridine, pyrazolo[1,5-a]pyrimidine, pyrazole, pyrazolopyridazine, dienamide, and pyranone derivatives. In-vitro cytotoxic screening was performed for all analogs against several human cancer cell lines. Compound 21 showed significant anti-breast cancer activity and a safety profile against the normal human cell lines (BJ-1). Furthermore, compound 21 was chosen as a representative example to study its potential apoptotic mechanism in the MCF-7 cancer cell line. It enhanced DNA fragmentation alongside its characteristic effect on tubulin polymerization. In addition, compound 21 up-regulated the pro-apoptotic Bax protein, decreased the Bcl-2 anti-apoptotic protein, and increased p53 and Caspase-7 levels confirming its mitochondrial intrinsic apoptotic activation.
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关键词
Anticancer activity,apoptotic proteins,dienamide,pyranone,pyrazolo[1,5-a]pyrimidine
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