상세 보기
Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors
- Chun, Kwangwoo;
- Park, Ji-Seon;
- Lee, Han-Chang;
- Kim, Young-Ha;
- Ye, In-Hea;
- ... Kim, Seung Hyun;
- 외 6명
Citations
WEB OF SCIENCE
16Citations
SCOPUS
17초록
New potent glycogen synthase kinase-3 (GSK-3) inhibitors, 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives, were designed by modeling, synthesized and evaluated in vitro. Compound 17c showed good potency in enzyme and cell-based assays (IC50 = 111 nM, EC50 = 1.78 mu M). Moreover, it has demonstrated desirable water solubility, PK profile, and moderate brain penetration.
키워드
Glycogen synthase kinase-3; GSK-3 inhibitor; 8-Amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives; ACTIVE-SITE; INDIRUBINS; DISCOVERY; DOCKING; POTENT; ROLES
- 제목
- Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors
- 저자
- Chun, Kwangwoo; Park, Ji-Seon; Lee, Han-Chang; Kim, Young-Ha; Ye, In-Hea; Kim, Kang-Jeon; Ku, Il-Whea; Noh, Min-Young; Cho, Goang-Won; Kim, Heejaung; Kim, Seung Hyun; Kim, Jeongmin
- 발행일
- 2013-07
- 유형
- Article
- 권
- 23
- 호
- 13
- 페이지
- 3983 ~ 3987