191729-02-9Relevant articles and documents
Synthesis of piperazine tethered 4-aminoquinoline-pyrimidine hybrids as potent antimalarial agents
Thakur, Anuj,Khan, Shabana I.,Rawat, Diwan S.
, p. 20729 - 20736 (2014)
A series of 4-aminoquinoline-pyrimidine hybrids linked through piperazine were synthesized and evaluated for their in vitro antimalarial activity against chloroquine (CQ)-sensitive and chloroquine (CQ)-resistant strains of Plasmodium falciparum and cytoto
Design, synthesis and biological evaluation of pyrimidine-based derivatives as VEGFR-2 tyrosine kinase inhibitors
Sun, Wuji,Hu, Shengquan,Fang, Shubiao,Yan, Hong
, p. 393 - 405 (2018/04/23)
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has already become an attractive approach for cancer therapy. In this study, a novel pyrimidine-based derivative 7j was designed as lead compound, and three series of potent VEGFR-2 inhibitors were synthesized and biologically evaluated against A549 and HepG2 cell lines. Compounds 7d, 9s and 13n exhibited superior inhibitory activities against A549 cell with IC50 ranged from 9.19 to 13.17 μM and HepG2 cell with IC50 ranged from 11.94 to 18.21 μM compared to those of Pazopanib (IC50 = 21.18 and 36.66 μM). In addition, molecular docking study was performed to investigate the binding capacity and binding mode between target compounds and VEGFR-2.
Novel CDK2 inhibitor and application thereof in resisting of breast cancer
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Paragraph 0041; 0044; 0048, (2018/05/16)
The invention relates to a CDK2 inhibitor and application thereof, belonging to the technical field of anti-tumor pharmacy. The invention provides a compound as the CDK2 inhibitor. The compound contains a compound represented by a formula (shown in the de