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Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors
- Title
- Design, synthesis, and evaluation of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives as Aurora kinase inhibitors
- Authors
- Jeong, Yunkyung; Lee, Jooyeon; Ryu, Jae-Sang
- Ewha Authors
- 류재상
- SCOPUS Author ID
- 류재상
- Issue Date
- 2016
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- ISSN
- 0968-0896
1464-3391
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY vol. 24, no. 9, pp. 2114 - 2124
- Keywords
- Aurora kinase; Click chemistry; Hinge-binder; 1,2,3-Triazole; Anticancer
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Indexed
- SCI; SCIE; SCOPUS
- Document Type
- Article
- Abstract
- A series of hinge-binder tethered 1,2,3-triazolylsalicylamide derivatives were designed, synthesized, and evaluated for the Aurora kinase inhibitory activities. The novel hinge-binder tethered 1,2,3-triazolylsalicylamide scaffold was effectively assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). A variety of alkynes with hinge binders were used to search proper structures-binding relationship to the hinge region. The synthesized 1,2,3-triazolylsalicylamide derivatives showed significant Aurora kinase inhibitory activity. In particular, 8a inhibited Aurora A kinase with an IC50 value of 0.284 mu M, whereas 8m inhibited Aurora B kinase with an IC50 value of 0.364 mu M. (C) 2016 Elsevier Ltd. All rights reserved.
- DOI
- 10.1016/j.bmc.2016.03.042
- Appears in Collections:
- 약학대학 > 약학과 > Journal papers
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