2. Academic Validation
  3. Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors

Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors

  • Eur J Med Chem. 2019 Feb 1:163:660-670. doi: 10.1016/j.ejmech.2018.12.025.
Seok Jong Kang 1,  Jung Wuk Lee 2,  Shin Hyuck Chung 2,  Sun Young Jang 1,  Jaeyul Choi 3,  Kwee Hyun Suh 3,  Young Hoon Kim 3,  Young Jin Ham 3,  Kyung Hoon Min 4
Affiliations

Affiliations

  • 1 College of Pharmacy, Chung-Ang University, Seoul, 06974, Republic of Korea; Department of Drug Discovery, Hanmi Research Center, Gyeonggi-do, 18469, Republic of Korea.
  • 2 College of Pharmacy, Chung-Ang University, Seoul, 06974, Republic of Korea.
  • 3 Department of Drug Discovery, Hanmi Research Center, Gyeonggi-do, 18469, Republic of Korea.
  • 4 College of Pharmacy, Chung-Ang University, Seoul, 06974, Republic of Korea. Electronic address: khmin@cau.ac.kr.
PMID: 30576901 DOI: 10.1016/j.ejmech.2018.12.025
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.

Keywords

Colon cancer; Imidazopyrazine; TAK1.

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