Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors
- Title
- Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors
- Author
- 하정미
- Keywords
- Aurora kinase; Click chemistry; Library; 1,2,3-Triazole; Anticancer
- Issue Date
- 2014-09
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v. 22, NO. 17, Page. 4855-4866
- Abstract
- A series of 1,2,3-triazolylsalicylamide derivatives has been developed from the antiproliferative agent 7 and was evaluated for their Aurora kinase inhibitory activity. The novel 1,2,3-triazolylsalicylamide scaffold could be readily assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition, allowing rapid access to the structurally diverse analogues. The synthesized 1,2,3-triazolylsalicylamide derivatives revealed a significant Aurora kinase inhibitory activity. In particular, 8g inhibited Aurora A with IC50 values of 0.37 mu M. The critical role of phenolic -OH in the binding was confirmed by a molecular modeling study. (C) 2014 Elsevier Ltd. All rights reserved.
- URI
- https://www.sciencedirect.com/science/article/pii/S0968089614004933?via%3Dihubhttps://repository.hanyang.ac.kr/handle/20.500.11754/186124
- ISSN
- 0968-0896;1464-3391
- DOI
- 10.1016/j.bmc.2014.06.047
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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