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Click approach to the discovery of 1,2,3-triazolylsalicylamides as potent Aurora kinase inhibitors
- Issue Date
- Sep-2014
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Aurora kinase; Click chemistry; Library; 1,2,3-Triazole; Anticancer
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY, v.22, no.17, pp.4855 - 4866
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY
- Volume
- 22
- Number
- 17
- Start Page
- 4855
- End Page
- 4866
- ISSN
- 0968-0896
- 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.
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Related Researcher
- Hah, Jung Mi
- COLLEGE OF PHARMACY (DEPARTMENT OF PHARMACY)