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Bioorg Med Chem Lett. 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.

Author information

1
Bristol-Myers Squibb, Rt. 206 & Province Line Road, Princeton, NJ 08540, USA. Electronic address: lan-ying.qin@bms.com.
2
Bristol-Myers Squibb, Rt. 206 & Province Line Road, Princeton, NJ 08540, USA.

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

PMID:
28108251
DOI:
10.1016/j.bmcl.2017.01.016
[Indexed for MEDLINE]

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