6289-87-8Relevant articles and documents
Designing and Accurately Developing a [6 + 2] Dipolar Cycloaddition for the Synthesis of Benzodiazocines
Cai, Wei,Chen, Kaihong,He, Yanlin,Huang, You,Yu, Cui,Zhou, Yiming
supporting information, p. 5430 - 5434 (2021/07/26)
1,6-Dipolar cycloadditions represent a valuable strategy for the rapid construction of medium-sized rings. Herein, we describe the concept for the design of 1,6-dipoles that bypasses the regioselectivity. Through the introduction of an amino group into Morita-Baylis-Hillman (MBH) carbonates, unprecedented [6 + 2] dipolar cycloadditions were accurately developed with Cs2CO3, efficiently delivering a series of benzodiazocines in mild conditions. Computational studies bring a deeper understanding of this reaction.
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.
Synthesis of 1-acyl-3,4-dihydroquinazoline-2(1H)-thiones by cyclization of N-[2-(isothiocyanatomethyl)phenyl] amides generated in situ from N-[2-(azidomethyl)phenyl] amides
Kobayashi, Kazuhiro,Matsumoto, Naoki
, p. 923 - 930 (2014/08/05)
An efficient method for the preparation of 1-acyl-3,4-dihydroquinazoline- 2(1H)-thiones 5 has been developed. The reaction of N-[2-(azidomethyl)phenyl] amides 3, easily prepared by a three-step sequence starting with (2-aminophenyl)methanols, with Ph