Bioorganic and Medicinal Chemistry Letters p. 855 - 861 (2017)
Update date:2022-08-03
Topics:
Qin, Lan-Ying
Ruan, Zheming
Cherney, Robert J.
Dhar, T.G. Murali
Neels, James
Weigelt, Carolyn A.
Sack, John S.
Srivastava, Anurag S.
Cornelius, Lyndon A.M.
Tino, Joseph A.
Stefanski, Kevin
Gu, Xiaomei
Xie, Jenny
Susulic, Vojkan
Yang, Xiaoxia
Yarde-Chinn, Melissa
Skala, Stacey
Bosnius, Ruth
Goldstein, Christine
Davies, Paul
Ruepp, Stefan
Salter-Cid, Luisa
Bhide, Rajeev S.
Poss, Michael A.
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.
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