Identification of highly potent and selective PI3Kδ inhibitors. Issue 13 (1st July 2017)

• Record Type: Journal Article
• Authors: Marcoux, David; Qin, Lan-Ying; Ruan, Zheming; Shi, Qing; Ruan, Qian; Weigelt, Carolyn; Qiu, Hongchen; Schieven, Gary; Hynes, John; Bhide, Rajeev; Poss, Michael; Tino, Joseph
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 13(2017)
• Page Start: 2849
• Page End: 2853
• Publication Date: 2017-07-01
• Subjects: PI3Kδ -- Pyrrolotriazine -- Autoimmune diseases -- Rheumatoid arthritis -- Phosphoinositide 3-kinases; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.01.077
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Selective PI3Kδ inhibitors have recently been hypothesized to be appropriate immunosuppressive agents for the treatment of immunological disorders such as rheumatoid arthritis. However, few reports have highlighted molecules that are highly selective for PI3Kδ over the other PI3K isoforms. In this letter, isoform and kinome selective PI3Kδ inhibitors are presented. The Structural Activity Relationship leading to such molecules is outlined.