Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors

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Title
Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors
Author(s)
Y An; E Lee; Y Yu; Ji Eun Yun; Myeong Youl LeeJong Soon Kang; W Y Kim; R Jeon
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 26, no. 13, pp. 3067-3072
Publication Year
2016
Abstract
A novel series of benzoxazole analogs was designed and synthesized, and their inhibitory activities against Aurora kinases were evaluated. Some of the tested compounds exhibited a promising activity with respect to the inhibition of Aurora B kinase. A structure-activity relationship study indicated that linker length, regiochemistry, and halogen substitution play important roles in kinase inhibitory potency. The binding modes between representative compounds and Aurora kinases were interpreted through a molecular docking study to explain the inhibitory activity and selectivity for Aurora A and B kinases. Compounds 13l and 13q also show an antiproliferative effect on the human tumor cell lines in a dose-dependent manner. The most potent 13q demonstrated good efficacy in the prostate cancer PC-3 tumor xenograft model.
Keyword
Aurora B kinaseBenzoxazole analogsAntiproliferation
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2016.05.017
Type
Article
Appears in Collections:
Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
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