Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists was written by Wijtmans, Maikel;Maussang, David;Sirci, Francesco;Scholten, Danny J.;Canals, Meritxell;Mujic-Delic, Azra;Chong, Milagros;Chatalic, Kristell L. S.;Custers, Hans;Janssen, Elwin;de Graaf, Chris;Smit, Martine J.;de Esch, Iwan J. P.;Leurs, Rob. And the article was included in European Journal of Medicinal Chemistry in 2012.Application of 25560-00-3 This article mentions the following:
The chemokine receptor CXCR7 is an atypical G protein-coupled receptor as it preferentially signals through the β-arrestin pathway rather than through G proteins. CXCR7 is thought to be of importance in cancer and the development of CXCR7-targeting ligands is of huge importance to further elucidate the pharmacol. and the therapeutic potential of CXCR7. In the present study, 24 derivatives were synthesized based on a compound scaffold patented by Chemocentryx and obtained CXCR7 ligands with pKi values ranging from 5.3 to 8.1. SAR studies were supported by computational 3D Fingerprint studies, revealing several important affinity descriptors. Two key compounds I and II (VUF11207 and VUF11403) were found to be high-potency ligands that induce recruitment of β-arrestin 2 and subsequent internalization of CXCR7, making them important tool compounds in future CXCR7 research. In the experiment, the researchers used many compounds, for example, 3-(2-Methylpiperidin-1-yl)propan-1-amine (cas: 25560-00-3Application of 25560-00-3).
3-(2-Methylpiperidin-1-yl)propan-1-amine (cas: 25560-00-3) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application of 25560-00-3
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem