Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors. Issue 13 (1st July 2016)

• Record Type: Journal Article
• Authors: An, Ying; Lee, Eun; Yu, Yeongji; Yun, Jieun; Lee, Myeong Youl; Kang, Jong Soon; Kim, Woo-Young; Jeon, Raok
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 13(2016)
• Page Start: 3067
• Page End: 3072
• Publication Date: 2016-07-01
• Subjects: Aurora B kinase -- Antiproliferation -- Benzoxazole analogs; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.05.017
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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. Compounds13l and13q also show an antiproliferative effect on the human tumor cell lines in a dose-dependent manner. The most potent13q demonstrated good efficacy in the prostate cancer PC-3 tumor xenograft model.