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Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors
- Authors
- Kang, Seok Jong; Lee, Jung Wuk; Chung, Shin Hyuck; Jang, Sun Young; Choi, Jaeyul; Suh, Kwee Hyun; Kim, Young Hoon; Ham, Young Jin; Min, Kyung Hoon
- Issue Date
- Feb-2019
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- Keywords
- TAK1; Imidazopyrazine; Colon cancer
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.163, pp 660 - 670
- Pages
- 11
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 163
- Start Page
- 660
- End Page
- 670
- ISSN
- 0223-5234
1768-3254
- Abstract
- Transforming growth factor-beta 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. (C) 2018 Elsevier Masson SAS. All rights reserved.
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