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Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors
- Cho, Sung Yun;
- Han, Sun-Young;
- Ha, Jae Du;
- Ryu, Jae Wook;
- Lee, Chong Ock;
- ... Lee, Jongkook;
- 외 4명
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We report the synthesis and biological evaluation of aminopyridines substituted with benzoxazole. The SAR of the aminopyridines was explored to improve the inhibitory activity against c-Met and to decrease hERG affinity. These studies led to the discovery of amide 24 which showed good c-Met inhibitory potency, low affinity to hERG and favorable pharmacokinetic properties in rats. (C) 2010 Elsevier Ltd. All rights reserved.
키워드
c-Met inhibitor; Aminopyridine; Benzoxazole; hERG; HEPATOCYTE GROWTH-FACTOR; MEDICINAL CHEMISTRY; HERG CHANNEL; RECEPTOR; CANCER; BLOCKADE; LIGANDS; DOMAIN
- 제목
- Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors
- 저자
- Cho, Sung Yun; Han, Sun-Young; Ha, Jae Du; Ryu, Jae Wook; Lee, Chong Ock; Jung, Heejung; Kang, Nam Sook; Kim, Hyoung Rae; Koh, Jong Sung; Lee, Jongkook
- 발행일
- 2010-07-15
- 유형
- Article
- 권
- 20
- 호
- 14
- 페이지
- 4223 ~ 4227