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
| Autor: | Anna Iatsyshyna, L. L. Lukash, Galyna P. Volynets, Sergiy M. Yarmoluk, Yaroslav V. Bilokin, Iryna Borysenko, Andrii Gryshchenko, S. S. Lukashov, Volodymyr G. Bdzhola, T. P. Ruban, Sergiy A. Starosyla |
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| Rok vydání: | 2019 |
| Předmět: |
chemistry.chemical_classification
010405 organic chemistry Chemistry Kinase Fibroblast growth factor receptor 1 Carboxylic acid General Chemistry 010402 general chemistry medicine.disease_cause 01 natural sciences In vitro 0104 chemical sciences Biochemistry medicine Carcinogenesis Protein kinase A IC50 |
| Zdroj: | Monatshefte für Chemie - Chemical Monthly. 150:1801-1808 |
| ISSN: | 1434-4475 0026-9247 |
| DOI: | 10.1007/s00706-019-02493-5 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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