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Lan-Ying Qin Zheming Ruan Robert J. Cherney T.G. Murali Dhar James Neels Carolyn A. Weigelt John S. Sack Anurag S. Srivastava Lyndon A.M. Cornelius Joseph A. Tino Kevin Stefanski Xiaomei Gu Jenny Xie Vojkan Susulic Xiaoxia Yang Melissa Yarde-Chinn Stacey Skala Ruth Bosnius Michael A. Poss 《Bioorganic & medicinal chemistry letters》2017,27(4):855-861
As demonstrated in preclinical animal models, the disruption of PI3Kδ expression or its activity leads to a decrease in inflammatory and immune responses. Therefore, inhibition of PI3Kδ may provide an alternative treatment for autoimmune diseases, such as RA, SLE, and respiratory ailments. Herein, we disclose the identification of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent, selective and orally bioavailable PI3Kδ inhibitors. The lead compound demonstrated efficacy in an in vivo mouse KLH model. 相似文献
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