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Kinase Inhibitors of Novel Pyridopyrimidinone Candidates: Synthesis and In Vitro Anticancer Properties
Joint Authors
Bakheit, Ahmed H.
Khalifa, Nagy M.
Alkahtani, Hamad M.
al-Omar, Mohamed A.
Source
Issue
Vol. 2019, Issue 2019 (31 Dec. 2019), pp.1-10, 10 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2019-03-20
Country of Publication
Egypt
No. of Pages
10
Main Subjects
Abstract EN
A new class of pyridopyrimidinone compounds containing different nitrogenous heterocycles were synthesized starting from the key precursor 2-hydrazinyl-5-phenyl-7-(pyridin-3-yl)pyrido[2,3-d]pyrimidin-4(3H)-one via condensation with series of aromatic aldehydes and cyclization using different reagents as ethyl acetoacetate, ethyl cyanoacetate, diethyl malonate, and ammonium isothiocyanate.
The bioassay results showed compound 6 to be highly effective towards three human cancer cell lines (HepG2, PC-3, and HCT-116) in vitro with promising activity values (IC50: 0.5 μM) relative to the standard doxorubicin (IC50: 0.6 μM).
Kinase inhibitory evaluation of compound 6 displays hopeful inhibitory action against BRAF V600E, EGFR, and PDGFRβ at100 μM.
The molecular docking studies supported the initial kinase assay.
American Psychological Association (APA)
Khalifa, Nagy M.& al-Omar, Mohamed A.& Alkahtani, Hamad M.& Bakheit, Ahmed H.. 2019. Kinase Inhibitors of Novel Pyridopyrimidinone Candidates: Synthesis and In Vitro Anticancer Properties. Journal of Chemistry،Vol. 2019, no. 2019, pp.1-10.
https://search.emarefa.net/detail/BIM-1170746
Modern Language Association (MLA)
Khalifa, Nagy M.…[et al.]. Kinase Inhibitors of Novel Pyridopyrimidinone Candidates: Synthesis and In Vitro Anticancer Properties. Journal of Chemistry No. 2019 (2019), pp.1-10.
https://search.emarefa.net/detail/BIM-1170746
American Medical Association (AMA)
Khalifa, Nagy M.& al-Omar, Mohamed A.& Alkahtani, Hamad M.& Bakheit, Ahmed H.. Kinase Inhibitors of Novel Pyridopyrimidinone Candidates: Synthesis and In Vitro Anticancer Properties. Journal of Chemistry. 2019. Vol. 2019, no. 2019, pp.1-10.
https://search.emarefa.net/detail/BIM-1170746
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1170746