177167-05-4Relevant articles and documents
Design, synthesis, biological evaluation of 6-(2-amino-1H-benzo[d]imidazole-6-yl)quinazolin-4(3H)-one derivatives as novel anticancer agents with Aurora kinase inhibition
Fan, Chengcheng,Fan, Yanhua,Wang, Daoping,Xu, Yongnan,Yang, Huarong,Yang, Xiaosheng,Yang, Ying,Zhong, Ting
, (2020)
Aurora A kinase, a member of the Aurora kinase family, is frequently overexpressed in various human cancers. In addition, Overexpression of Aurora A kinase is associated with drug resistance and poor prognosis in many cancers including breast cancer. Therefore, Aurora A kinase has been considered as an attractive anticancer target for the treatment of human cancers. Herein, A series of 6-(2-amino-1H-benzo[d]imidazole-6-yl)quinazolin-4(3H)-one derivatives were designed, synthesized, and evaluated as Aurora A kinase inhibitors. The cell-based cytotoxicity assays showed that compound 16h was the most potent cytotoxic agent against all tested cancer cells and had a lower IC50 value than ENMD-2076 against MDA-MB-231 cells. Meanwhile, Aurora A kinase assay and Western blot analysis showed that 16h inhibited Aurora A kinase with an IC50 value of 21.94 nM and suppressed the phosphorylation of Histone H3 on Ser10 and Aurora A kinase on Thr288, which were consistent with the activation of Aurora A kinase. Accordingly, 16h caused aberrant mitotic phenotypes and obvious G2/M phase arrest in MDA-MB-231 cells and induced caspase-dependent apoptosis in MDA-MB-231 cells. These results demonstrated that 16h is a potential candidate for the development of anticancer agents targeting Aurora A kinase.
Pyrido imidazole substituted quinazolinone derivative as well as synthesis method and application thereof
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Paragraph 0063-0064, (2021/10/16)
The invention discloses a pyridazole substituted quinazolinone derivative, and the structural formula thereof is as follows. The invention also discloses a synthetic method thereof. The pyrido-imidazole-substituted quinazolinone derivative can induce high
QUINAZOLINE BASED RESPIRATORY SYNCYTIAL VIRUS INHIBITORS
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Page/Page column 53, (2015/05/19)
Compounds of Formula (I), wherein R1, R2, R3, R4 and n are defined herein, are useful as inhibitors of RSV.