Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors
- Authors
- An, Ying; Lee, Eun; Yu, Yeongji; Yun, Jieun; Lee, Myeong Youl; Kang, Jong Soon; Kim, Woo-Young; Jeon, Raok
- Issue Date
- Jul-2016
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Aurora B kinase; Antiproliferation; Benzoxazole analogs
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.26, no.13, pp 3067 - 3072
- Pages
- 6
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 26
- Number
- 13
- Start Page
- 3067
- End Page
- 3072
- URI
- https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/9717
- DOI
- 10.1016/j.bmcl.2016.05.017
- ISSN
- 0960-894X
1464-3405
- 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. (C) 2016 Elsevier Ltd. All rights reserved.
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