Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors.

ID: ALA4411291

Journal: Eur J Med Chem

Title: Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors.

Authors: Kang SJ, Lee JW, Chung SH, Jang SY, Choi J, Suh KH, Kim YH, Ham YJ, Min KH.

Abstract: Transforming growth factor-β activated kinase-1 (TAK1) is a potential therapeutic target for cancers and inflammatory diseases. We synthesized a series of novel imidazopyrazine derivatives, which were found to exhibit potent inhibitory effect against TAK1. Compound 22a, which possesses a good pharmacokinetic profile, showed excellent in vitro kinase activity and significant in vivo efficacy in mice xenografted with SW620, a KRAS-dependent colon cancer cell line.

CiteXplore: 30576901

DOI: 10.1016/j.ejmech.2018.12.025

Patent ID: ┄