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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, YunkyungLee, JooyeonRyu, Jae-Sang
Ewha Authors
류재상
SCOPUS Author ID
류재상scopus
Issue Date
2016
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN
0968-0896JCR Link1464-3391JCR Link
Citation
vol. 24, no. 9, pp. 2114 - 2124
Keywords
Aurora kinaseClick chemistryHinge-binder1,2,3-TriazoleAnticancer
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Indexed
SCI; SCIE; SCOPUS WOS scopus
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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