Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2017 Jul 1;27(13):2849-2853. doi: 10.1016/j.bmcl.2017.01.077. Epub 2017 Feb 7.

Identification of highly potent and selective PI3Kδ inhibitors.

Author information

1
Research & Development, Bristol-Myers Squibb Company, Route 206 & Province Line Road, Princeton, NJ 08543, United States. Electronic address: david.marcoux@bms.com.
2
Research & Development, Bristol-Myers Squibb Company, Route 206 & Province Line Road, Princeton, NJ 08543, United States.

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.

KEYWORDS:

Autoimmune diseases; PI3Kδ; Phosphoinositide 3-kinases; Pyrrolotriazine; Rheumatoid arthritis

PMID:
28209465
DOI:
10.1016/j.bmcl.2017.01.077
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center