Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships
| Autor: | Maria Gabriella Brasca, Nicoletta Colombo, Francesco Sola, Ermes Vanotti, Sandrine Thieffine, Barbara Valsasina, Daniele Volpi, Alberto Bargiotti, Antonella Ermoli, Marcellino Tibolla, Federico Riccardi Sirtori, Maria Menichincheri, Antonio Pillan, Gabriele Fachin, Antonella Ciavolella, Alessia Montagnoli, Sonia Rainoldi, Antonella Isacchi, Antonio Molinari, Corrado Santocanale |
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| Přispěvatelé: | Ermoli, A, Bargiotti, A, Brasca, M, Ciavolella, A, Colombo, N, Fachin, G, Isacchi, A, Menichincheri, M, Molinari, A, Montagnoli, A, Pillan, A, Rainoldi, S, Sirtori, F, Sola, F, Thieffine, S, Tibolla, M, Valsasina, B, Volpi, D, Santocanale, C, Vanotti, E |
| Jazyk: | angličtina |
| Rok vydání: | 2009 |
| Předmět: |
Models
Molecular chemistry.chemical_classification Pyridines Kinase Stereochemistry Molecular Conformation Cell Cycle Proteins Protein Serine-Threonine Kinases Chemical synthesis In vitro Cell Line Cell division cycle Structure-Activity Relationship chemistry.chemical_compound Enzyme chemistry Biochemistry Cell culture Drug Discovery Pyridine Humans Molecular Medicine Structure–activity relationship kinase inhibitors Protein Kinase Inhibitors |
| Popis: | Cdc7 kinase has recently emerged as an attractive target for cancer therapy and low-molecular-weight inhibitors of Cdc7 kinase have been found to be effective in the inhibition of tumor growth in animal models. In this paper, we describe synthesis and structure-activity relationships of new 1H-pyrrolo[2,3-b]pyridine derivatives identified as inhibitors of Cdc7 kinase. Progress from (Z)-2-phenyl-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-3,5-dihydro-4H-imidazol-4-one (1) to [(Z)-2-(benzylamino)-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-1,3-thiazol-4(5H)-one] (42), a potent ATP mimetic inhibitor of Cdc7 kinase with IC(50) value of 7 nM, is also reported. |
| Databáze: | OpenAIRE |
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