Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2013 Aug 15;23(16):4517-22.
doi: 10.1016/j.bmcl.2013.06.053. Epub 2013 Jun 25.

Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1

Keith R Hornberger  1 , Dan M Berger, Andrew P Crew, Hanqing Dong, Andrew Kleinberg, An-Hu Li, Matthew R Medeiros, Mark J Mulvihill, Kam Siu, James Tarrant, Jing Wang, Felix Weng, Victoria L Wilde, Mark Albertella, Mark Bittner, Andrew Cooke, Michael J Gray, Paul Maresca, Earl May, Peter Meyn, William Peick Jr, Darlene Romashko, Michael Tanowitz, Brianna Tokar
Affiliations

Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1

Keith R Hornberger et al. Bioorg Med Chem Lett. .

Abstract

The discovery and potency optimization of a series of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1 is described. Micromolar hits taken from high-throughput screening were optimized for biochemical and cellular mechanistic potency to ~10nM, as exemplified by compound 12az. Application of structure-based drug design aided by co-crystal structures of TAK1 with inhibitors significantly shortened the number of iterations required for the optimization.

Keywords: 7-Amino-furo[2,3-c]pyridine; Cancer; Inflammation; Inhibitors; TAK1.

PubMed Disclaimer

MeSH terms

LinkOut - more resources