1007660-74-3Relevant academic research and scientific papers
Identification of protein kinase fibroblast growth factor receptor 1 (FGFR1) inhibitors among the derivatives of 5-(5,6-dimethoxybenzimidazol-1-yl)-3-hydroxythiophene-2-carboxylic acid
Volynets, Galyna,Lukashov, Sergiy,Borysenko, Iryna,Gryshchenko, Andrii,Starosyla, Sergiy,Bdzhola, Volodymyr,Ruban, Tetiana,Iatsyshyna, Anna,Lukash, Lyubov,Bilokin, Yaroslav,Yarmoluk, Sergiy
, p. 1801 - 1808 (2019/11/05)
Abstract: Fibroblast growth factor receptor 1 (FGFR1) plays an important role in tumorigenesis, suggesting that inhibitors of this protein kinase may become important compounds for the development of anticancer agents. Using molecular docking approach, we have identified a novel class of FGFR1 inhibitors belonging to the derivatives of 5-(5,6-dimethoxybenzimidazol-1-yl)-3-hydroxythiophene-2-carboxylic acid. It was revealed that the most promising compound 5-(5,6-dimethoxybenzimidazol-1-yl)-3-[2-(methanesulfonyl)benzyloxy]thiophene-2-carboxylic acid methyl ester inhibits FGFR1 with an IC50 value of 150?nM in in vitro kinase assay. The structure–activity relationships have been studied, and the binding mode of this chemical class has been proposed. Graphic abstract: [Figure not available: see fulltext.]
Discovery of thiophene inhibitors of polo-like kinase
Emmitte, Kyle A.,Andrews, C. Webb,Badiang, Jennifer G.,Davis-Ward, Ronda G.,Dickson, Hamilton D.,Drewry, David H.,Emerson, Holly K.,Epperly, Andrea H.,Hassler, Daniel F.,Knick, Victoria B.,Kuntz, Kevin W.,Lansing, Timothy J.,Linn, James A.,Mook Jr., Robert A.,Nailor, Kristen E.,Salovich, James M.,Spehar, Glenn M.,Cheung, Mui
scheme or table, p. 1018 - 1021 (2009/09/06)
The discovery and development of a series of thiophenes as potent and selective inhibitors of PLK is described. Identification and characterization of 2, a useful in vitro PLK inhibitor tool compound, is also presented.
