Design, Synthesis, and Characterization of Novel CXCR4 Antagonists Featuring Cyclic Amines was written by Lin, Yu;Li, Zhanhui;Ma, Haikuo;Wang, Yujie;Wang, Xu;Song, Shiwei;Zhao, Li;Wu, Shuwei;Tian, Sheng;Fu, Chunyan;Luo, Lusong;Zhu, Fang;He, Sudan;Zheng, Jiyue;Zhang, Xiaohu. And the article was included in ChemMedChem in 2020.Recommanded Product: Ethyl 4-chloro-3-oxobutanoate The following contents are mentioned in the article:
Chemokine receptor CXCR4 and its natural ligand CXCL12 (also known as stromal cell-derived factor-1, or SDF-1) regulate a broad range of physiol. functions. Dysregulation of the CXCL12/CXCR4 axis is involved in numerous pathol. 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(I) 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 crystallog. This study involved multiple reactions and reactants, such as Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3Recommanded Product: Ethyl 4-chloro-3-oxobutanoate).
Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3) belongs to organic chlorides. Chlorinated organic compounds are found in nearly every class of biomolecules and natural products including alkaloids, terpenes, amino acids, flavonoids, steroids, and fatty acids. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Recommanded Product: Ethyl 4-chloro-3-oxobutanoate
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics