1605398-18-2Relevant academic research and scientific papers
A pyrimidine compound and its preparation method and application
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Paragraph 0055-0060, (2019/06/26)
The invention discloses a pyrimidine compound and a synthesis method and application thereof. The pyrimidine compound has the structural general formula represented by a formula shown in descriptions. The pyrimidine compound disclosed by the invention can be used for excellently inhibiting the activity of Aurora kinase, can be used as an Aurora kinase activity inhibitor for experiments, and is expected to be developed into drugs for treating leukemia. According to the pyrimidine compound disclosed by the invention, synthesis steps are relatively simple, and the production cost is relatively low, so that industrial production is facilitated.
Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors
Luo, Yu,Deng, Yan-Qiu,Wang, Jing,Long, Zi-Jie,Tu, Zheng-Chao,Peng, Wei,Zhang, Ji-Quan,Liu, Quentin,Lu, Gui
supporting information, p. 65 - 71 (2014/04/17)
The design and synthesis of a new series of N-trisubstituted (at C2, C4 and C6 respectively) pyrimidine derivatives were reported, their in vitro structure-activity relationships vs. aurora A kinase were also discussed. Our results demonstrated that the introduction of characteristic N-substituted side chain at C2 of pyrimidines possessed a potent aurora A inhibitory activity, the position and the nature of the substituents on the phenyl ring of aniline side chain played key roles in cellular kinase inhibitory potency. Most tested compounds exhibited good inhibitory activities against aurora A kinase and various human tumor cell lines. Compounds 7j, 7m-n and 7p showed strong growth-inhibitory activities in the solid CNE-2 tumor cell and selectively blocked cell-cycle progression at the G2/M phase.
