216574-71-9Relevant academic research and scientific papers
Microwave-assisted synthesis of 2-aminothiophene derivatives via improved gewald reactions
Ruan, Bankang,Zhang, Zhiyan,Huang, Lei,Xu, Chao,Li, Luolan
, p. 2007 - 2018 (2021/09/29)
In this paper, a new and efficient method was developed to prepare 2-aminothiophene derivatives through improved Gewald reaction. Thirty-one final products were synthesized under microwave radiation for 30 min with 57%-95% isolated yields. All the product
Potent and selective thiophene urea-templated inhibitors of S6K
Ye, Ping,Kuhn, Cyrille,Juan, Miret,Sharma, Rahul,Connolly, Brendan,Alton, Gordon,Liu, Hu,Stanton, Robert,Kablaoui, Natasha M.
experimental part, p. 849 - 852 (2011/03/18)
S6K1 (p70 S6 kinase-1) is thought to play a critical role in the development of obesity and insulin resistance, thus making it an attractive target in developing medicines for the treatment of these disorders. We describe a novel thiophene urea class of S6K inhibitors. The lead matter for the development of these inhibitors came from mining the literature for reports of weak off-target S6K activity. These optimized inhibitors exhibit good potency and excellent selectivity for S6K over a panel of 43 kinases.
UREA INHIBITORS OF MAP KINASES
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Page/Page column 20, (2010/03/04)
Urea containing compounds that inhibit MAP kinases, pharmaceutical compositions including such compounds and methods for using these compounds to treat inflammatory diseases and cancer are described herein.
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation and structure-activity relationships. Part 2
Horiuchi, Takao,Nagata, Motoko,Kitagawa, Mayumi,Akahane, Kouichi,Uoto, Kouichi
experimental part, p. 7850 - 7860 (2010/04/02)
The design, synthesis and evaluation of novel thieno[2,3-d]pyrimidin-4-yl hydrazone analogues as cyclin-dependent kinase 4 (CDK4) inhibitor are described. Focusing on the optimization of the heteroaryl moiety at the hydrazone with substituted phenyl group
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: Synthesis, biological evaluation, and structure-activity relationships
Horiuchi, Takao,Chiba, Jun,Uoto, Kouichi,Soga, Tsunehiko
scheme or table, p. 305 - 308 (2011/02/28)
The synthesis and evaluation of new analogues of thieno[2,3-d]pyrimidin-4-yl hydrazones are described. 2-Pyrdinecarboxaldehyde [6-(tert-butyl)thieno[2,3-d]pyrimidine-4-yl]hydrazone derivatives have been identified as cyclin-dependent kinase 4 (CDK4) inhibitors. The potency, selectivity profile, and structure-activity relationship of this series of compounds are discussed.
RAF KINASE INHIBITORS
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Page/Page column 25-26, (2008/12/06)
Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
Inhibition of p38 kinase activity by aryl ureas
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, (2008/06/13)
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases other than cancer and proteolytic enzyme mediated diseases other than cancer, and pharmaceutical compositions for use in such therapy.
Inhibition of raf kinase activity using aryl ureas
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, (2008/06/13)
Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
