89639-37-2Relevant articles and documents
Design, Synthesis, and Characterization of Novel CXCR4 Antagonists Featuring Cyclic Amines
Fu, Chunyan,He, Sudan,Li, Zhanhui,Lin, Yu,Luo, Lusong,Ma, Haikuo,Song, Shiwei,Tian, Sheng,Wang, Xu,Wang, Yujie,Wu, Shuwei,Zhang, Xiaohu,Zhao, Li,Zheng, Jiyue,Zhu, Fang
, (2020/06/01)
Chemokine receptor CXCR4 and its natural ligand CXCL12 (also known as stromal cell-derived factor-1, or SDF-1) regulate a broad range of physiological functions. Dysregulation of the CXCL12/CXCR4 axis is involved in numerous pathological conditions such as HIV infection, inflammation and cancer. Herein, we report the design, synthesis, and characterization of novel CXCR4 antagonists based on cyclic amine scaffolds. Compound 24 was identified as a potent CXCR4 receptor antagonist (competitive inhibition of 12G5 binding, IC50=24 nM; functional inhibition of CXCL12-induced cytosolic calcium increase, IC50=0.1 nM). In addition, compound 24 potently inhibited cell migration in CXCR4/CXCL12-mediated chemotaxis in a matrigel invasion assay. The absolute configuration of compound 24 was elucidated by X-ray crystallography.
HETEROARYL COMPOUNDS AS CXCR4 INHIBITORS, COMPOSITION AND METHOD USING THE SAME
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Paragraph 00181-00183, (2019/04/16)
The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to the CXCR4 pathway.
COMPOUNDS 947
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Page/Page column 115, (2009/03/07)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of proliferative disease such as cancer and partic
