PI3K Inhibitors of Novel Hydrazide Analogues Linked 2-Pyridinyl Quinazolone Scaffold as Anticancer Agents

作者: Ibrahim F. Zeid , Neama A. Mohamed , Nagy M. Khalifa , Emad M. Kassem , Eman S. Nossier

DOI: 10.1155/2019/6321573

关键词:

摘要: A series of novel 2-(pyridin-4-yl)quinazolin-4(3H)-ones bearing different heterocycle cores as potential PI3K inhibitors have been synthesized and evaluated via the MTT assay for their antiproliferative properties against selected HePG-2, MCF-7, HCT116 cancer cell lines. Among them, compound 9 displayed significant activity HePG-2 (IC50 = 60.29 ± 1.06 μM) comparable to doxorubicin a reference anticancer drug 69.60 1.50 μM). Kinase inhibitory assessment target products docking studies revealed promising binding affinities which match with mode ligand, SW13 towards active site PI3K. Therefore, this work represents matrix developing candidates.

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