Design, synthesis and anticancer activity of 2-arylimidazo[1,2-a]pyridinyl-3-amines

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dc.contributor.authorYadav, Umesh Prasad
dc.contributor.authorAnsari, Arshad J.
dc.contributor.authorArora, Sahil
dc.contributor.authorJoshi, Gaurav
dc.contributor.authorSingh, Tashvinder
dc.contributor.authorKaur, Harsimrat
dc.contributor.authorDogra, Nilambra
dc.contributor.authorKumar, Raj
dc.contributor.authorKumar, Santosh
dc.contributor.authorSawant, Devesh M.
dc.contributor.authorSingh, Sandeep
dc.date.accessioned2024-01-21T10:38:18Z
dc.date.accessioned2024-08-13T12:05:13Z
dc.date.available2024-01-21T10:38:18Z
dc.date.available2024-08-13T12:05:13Z
dc.date.issued2021-11-01T00:00:00
dc.description.abstractA series of imido-heterocycle compounds were designed, synthesized, characterized, and evaluated for the anticancer potential using breast (MCF-7 and MDA-MB-231), pancreatic (PANC-1), and colon (HCT-116 and HT-29) cancer cell lines and normal cells, while normal cells showed no toxicity. Among the screened compounds, 4h exhibited the best anticancer potential with IC50 values ranging from 1 to 5.5 ?M. Compound 4h caused G2/M phase arrest and apoptosis in all the cell lines except MDA-MB-231 mammosphere formation was inhibited. In-vitro enzyme assay showed selective topoisomerase II? inhibition by compound 4h, leading to DNA damage as observed by fluorescent staining. Cell signalling studies showed decreased expression of cell cycle promoting related proteins while apoptotic proteins were upregulated. Interestingly MDA-MB-231 cells showed only cytostatic effects upon treatment with compound 4h due to defective p53 status. Toxicity study using overexpression of dominant-negative mutant p53 in MCF-7 cells (which have wild type functional p53) showed that anticancer potential of compound 4h is positively correlated with p53 expression. � 2021 Elsevier Inc.en_US
dc.identifier.doi10.1016/j.bioorg.2021.105464
dc.identifier.issn452068
dc.identifier.urihttp://10.2.3.109/handle/32116/3525
dc.identifier.urlhttps://linkinghub.elsevier.com/retrieve/pii/S0045206821008427
dc.language.isoen_USen_US
dc.publisherAcademic Press Inc.en_US
dc.subject2-Arylimidazo[1,2-a]pyridinyl-3-aminesen_US
dc.subjectAnticanceren_US
dc.subjectp53en_US
dc.subjectTopoisomerase inhibitorsen_US
dc.subjectWestern blottingen_US
dc.titleDesign, synthesis and anticancer activity of 2-arylimidazo[1,2-a]pyridinyl-3-aminesen_US
dc.title.journalBioorganic Chemistryen_US
dc.typeArticleen_US
dc.type.accesstypeClosed Accessen_US

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