Synthesis, modeling and functional activity of substituted styrene-amides as small-molecule CXCR7 agonists

…, DJ Scholten, M Canals, A Mujić-Delić, M Chong…

Index: 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 European Journal of Medicinal Chemistry, 2012 , vol. 51, p. 184 - 192

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Citation Number: 17

Abstract

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 pharmacology and the therapeutic potential of CXCR7. In the present study, we synthesized 24 derivatives based on a compound scaffold patented ...