Design, synthesis, and structure-activity relationship of novel RIPK2 inhibitors

The derivative 17 is obtained from the prodrug 5 (GSK2983559) by using a cyclization strategy and structural optimization. Compound 17 displays a high affinity for RIPK2 (Kd = 5.9 nM) and no affinity for RIPK1 (Kd > 30000 nM). Compound 17 exhibits favorable in vitro safety profiles and significan...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2022-11, Vol.75, p.128968-128968, Article 128968
Hauptverfasser:	Wu, Shuwei, Xu, Liben, Wang, Xinhui, Yang, Qing, Wang, Jingrui, He, Sudan, Zhang, Xiaohu
Format:	Artikel
Sprache:	eng
Schlagworte:	autoimmune disorders inhibitor Kinase NOD RIPK2
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