Pyrimidine containing epidermal growth factor receptor kinase inhibitors: Synthesis and biological evaluation

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dc.contributor.authorJoshi, Gaurav
dc.contributor.authorNayyar, Himanshu
dc.contributor.authorKalra, Sourav
dc.contributor.authorSharma, Praveen
dc.contributor.authorMunshi, Anjana
dc.contributor.authorSingh, Sandeep
dc.contributor.authorKumar, Raj
dc.date.accessioned2017-08-03T09:10:58Z
dc.date.accessioned2024-08-13T12:05:44Z
dc.date.available2017-08-03T09:10:58Z
dc.date.available2024-08-13T12:05:44Z
dc.date.issued2017
dc.description.abstractStructure-based design and synthesis of pyrimidine containing reversible epidermal growth factor receptor (EGFR) inhibitors 1a?d are reported. The compounds (1a?d) inhibited the EGFR kinase activity in vitro with IC50 range 740?nm to 3??m. mRNA expression of EGFR downstream target genes, that is twist, c-fos and aurora were found to be altered upon treatment with compounds 1a?d. The compounds 1a?d exhibited excellent anticancer activity at low micromolar level (3.2?9??m) in lung, colon and breast cancer cell lines. Furthermore, compounds induced the alteration in mitochondrial membrane potential and reactive oxygen species level and. Selected compound 1b was found to increase sub-G1 population indicative of cell death, the mode of cell death was apoptotic as evident from Annexin V verses propidium iodide assay. Molecular modelling further helped to investigate the binding recognition pattern of the compounds in ATP binding EGFR domain similar to erlotinib and dissimilar to WZ4002. ? 2017 John Wiley & Sons A/S.en_US
dc.identifier.citationJoshi, G., Nayyar, H., Kalra, S., Sharma, P., Munshi, A., Singh, S., & Kumar, R. (2017). Pyrimidine containing epidermal growth factor receptor kinase inhibitors: Synthesis and biological evaluation. Chemical Biology and Drug Design, 90(5), 995-1006. doi: 10.1111/cbdd.13027en_US
dc.identifier.doi10.1111/cbdd.13027
dc.identifier.issn17470277
dc.identifier.urihttp://10.2.3.109/handle/32116/277
dc.identifier.urlhttps://onlinelibrary.wiley.com/doi/abs/10.1111/cbdd.13027
dc.language.isoenen_US
dc.publisherBlackwell Publishing Ltden_US
dc.subjectPyrimidineen_US
dc.subjectReactive oxygen metaboliteen_US
dc.subjectUnclassified drugen_US
dc.subjectAntineoplastic agenten_US
dc.subjectEpidermal growth factor receptoren_US
dc.subjectProtein kinase inhibitoren_US
dc.subjectPyrimidineen_US
dc.titlePyrimidine containing epidermal growth factor receptor kinase inhibitors: Synthesis and biological evaluationen_US
dc.title.journalChemical Biology and Drug Design
dc.typeArticleen_US

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