1201939-89-0Relevant articles and documents
Quinolone antibiotic derivatives as new selective Axl kinase inhibitors
Tan, Li,Zhang, Zhang,Gao, Donglin,Chan, Shingpan,Luo, Jinfeng,Tu, Zheng-Chao,Zhang, Zhi-Min,Ding, Ke,Ren, Xiaomei,Lu, Xiaoyun
, p. 318 - 327 (2019)
Axl is a new promising molecular target for antineoplastic therapies. A series of quinolone antibiotic derivatives were designed and synthesized as new selective Axl inhibitors. One of the most promising compound 8i bound tightly to Axl with a Kd value of 1.1 nM, and inhibited its kinase activity with an IC50 value of 26 nM. The compound also significantly inhibited the phosphorylation of Axl and dose dependently inhibited cell invasion and migration in TGF-β1 induced MDA-MD-231 breast cancer cells. In addition, 8i demonstrated reasonable pharmacokinetic properties and exhibited extraordinary target selectivity over 468 kinases except for Flt3 (IC50 = 50 nM)), with a S(10) and S(35) value of 0.022 and 0.42 at 1.0 μM, respectively. Compound 8i may serve as a new valuable lead compound for future anticancer drug discovery.
Structure–activity relationship study of novel quinazoline-based 1,6-naphthyridinones as MET inhibitors with potent antitumor efficacy
Zhuo, Lin-Sheng,Wu, Feng-Xu,Wang, Ming-Shu,Xu, Hong-Chuang,Yang, Fan-Peng,Tian, Yan-Guang,Zhao, Xing-E.,Ming, Zhi-Hui,Zhu, Xiao-Lei,Hao, Ge-Fei,Huang, Wei
, (2020/09/09)
As a privileged scaffold, the quinazoline ring is widely used in the development of EGFR inhibitors, while few quinazoline-based MET inhibitors are reported. In our ongoing efforts to develop new MET-targeted anticancer drug candidates, a series of quinaz
A pyrazolo pyrimidine derivative and its preparation method and in the preparation of medicaments (by machine translation)
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Paragraph 0023; 0024; 0027; 0028; 0031; 0032, (2019/04/26)
The invention relates to the technical field of drugs, in particular a pyrazolo pyrimidine derivative and its preparation method and in the preparation of medicaments. The pyrimidine derivatives of formula I and states the pyrazole is shown: The present