Cargando…
7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent
Introduction of a 1-benzyl-1H-pyrazol-4-yl moiety at C7 of the imidazo[4,5-b]pyridine scaffold provided 7a which inhibited a range of kinases including Aurora-A. Modification of the benzyl group in 7a, and subsequent co-crystallisation of the resulting analogues with Aurora-A indicated distinct diff...
Autores principales: | Bavetsias, Vassilios, Pérez-Fuertes, Yolanda, McIntyre, Patrick J., Atrash, Butrus, Kosmopoulou, Magda, O’Fee, Lisa, Burke, Rosemary, Sun, Chongbo, Faisal, Amir, Bush, Katherine, Avery, Sian, Henley, Alan, Raynaud, Florence I., Linardopoulos, Spiros, Bayliss, Richard, Blagg, Julian |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier Science Ltd
2015
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4577729/ https://www.ncbi.nlm.nih.gov/pubmed/26296477 http://dx.doi.org/10.1016/j.bmcl.2015.08.003 |
Ejemplares similares
-
Aurora Isoform Selectivity:
Design and Synthesis of
Imidazo[4,5-b]pyridine Derivatives as Highly
Selective Inhibitors of Aurora-A Kinase in Cells
por: Bavetsias, Vassilios, et al.
Publicado: (2013) -
Optimization of Imidazo[4,5-b]pyridine-Based Kinase Inhibitors: Identification of a
Dual FLT3/Aurora
Kinase Inhibitor as an Orally Bioavailable Preclinical Development
Candidate for the Treatment of Acute Myeloid Leukemia
por: Bavetsias, Vassilios, et al.
Publicado: (2012) -
Metabolism of the dual FLT-3/Aurora kinase inhibitor CCT241736 in preclinical and human in vitro models: Implication for the choice of toxicology species
por: Wood, Francesca L., et al.
Publicado: (2019) -
Aurora Kinase Inhibitors: Current Status and Outlook
por: Bavetsias, Vassilios, et al.
Publicado: (2015) -
New Series of Pyrazoles and Imidazo-Pyrazoles Targeting Different Cancer and Inflammation Pathways
por: Signorello, Maria Grazia, et al.
Publicado: (2021)