Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors

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

doi:10.1016/j.ejmech.2018.12.025

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Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors

Kang, Seok Jong;
Lee, Jung Wuk;
Chung, Shin Hyuck;
Jang, Sun Young;
Choi, Jaeyul;
... Min, Kyung Hoon;
외 3명

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11

초록

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.

키워드

TAK1; Imidazopyrazine; Colon cancer; ACTIVATED KINASE 1; I-KAPPA-B; DISCOVERY; PROTEIN; MAPKKK; VITRO; IL-1; IDENTIFICATION; OPTIMIZATION; MUTATIONS

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

저자: 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

DOI: 10.1016/j.ejmech.2018.12.025

발행일: 2019-02

유형: Article

저널명: European Journal of Medicinal Chemistry

권: 163

페이지: 660 ~ 670

언어: ENG

출판사: ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER

발행국가: 프랑스

분량: 11 페이지

ISSN: E 1768-3254
P 0223-5234