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. 2017 Feb 15;27(4):855-861.
doi: 10.1016/j.bmcl.2017.01.016. Epub 2017 Jan 10.

Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors

Lan-Ying Qin  1 , Zheming Ruan  2 , Robert J Cherney  2 , T G Murali Dhar  2 , James Neels  2 , Carolyn A Weigelt  2 , John S Sack  2 , Anurag S Srivastava  2 , Lyndon A M Cornelius  2 , Joseph A Tino  2 , Kevin Stefanski  2 , Xiaomei Gu  2 , Jenny Xie  2 , Vojkan Susulic  2 , Xiaoxia Yang  2 , Melissa Yarde-Chinn  2 , Stacey Skala  2 , Ruth Bosnius  2 , Christine Goldstein  2 , Paul Davies  2 , Stefan Ruepp  2 , Luisa Salter-Cid  2 , Rajeev S Bhide  2 , Michael A Poss  2
Affiliations

Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors

Lan-Ying Qin et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: 7-Phenylpyrrolo[2,1-f][1,2,4]triazin-4-amine; Autoimmune diseases; PI3Kδ; Phosphoinositide 3-kinases; Rheumatoid arthritis.

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