26579-29-3Relevant academic research and scientific papers
Design and synthesis of novel benzoxazole analogs as Aurora B kinase inhibitors
An, Ying,Lee, Eun,Yu, Yeongji,Yun, Jieun,Lee, Myeong Youl,Kang, Jong Soon,Kim, Woo-Young,Jeon, Raok
, p. 3067 - 3072 (2016/06/13)
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.
