Structure Activity Relationship Studies around DB18, a Potent and Selective Inhibitor of CLK Kinases

Three series of our lead CLK1 inhibitor DB18 have been designed, synthetized and tested against CLKs and DYRK1A kinases. Their cytotoxicity was subsequently measured on seven representative cancer cell lines. Guided by docking experiments, we focused on the less constrained part of the scaffold, and...

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Detalles Bibliográficos
Autores principales: Brahmaiah, Dabbugoddu, Bhavani, Anagani Kanaka Durga, Aparna, Pasula, Kumar, Nangunoori Sampath, Solhi, Hélène, Le Guevel, Rémy, Baratte, Blandine, Robert, Thomas, Ruchaud, Sandrine, Bach, Stéphane, Jadav, Surender Singh, Reddy, Chada Raji, Mosset, Paul, Gouault, Nicolas, Levoin, Nicolas, Grée, René
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9571063/
https://www.ncbi.nlm.nih.gov/pubmed/36234686
http://dx.doi.org/10.3390/molecules27196149

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