Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation

Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation

Haspin is a mitotic protein kinase required for proper cell division by modulating Aurora B kinase localisation and activity as well as histone phosphorylation. Here a series of imidazopyridazines based on the CHR-6494 and Structure Activity Relationship was established. An assessment of the inhibit...

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Bibliographic Details
Main Authors: Jonathan Elie, Omid Feizbakhsh, Nathalie Desban, Béatrice Josselin, Blandine Baratte, Amandine Bescond, Julien Duez, Xavier Fant, Stéphane Bach, Dominique Marie, Matthieu Place, Sami Ben Salah, Agnes Chartier, Sabine Berteina-Raboin, Apirat Chaikuad, Stefan Knapp, Fabrice Carles, Pascal Bonnet, Frédéric Buron, Sylvain Routier, Sandrine Ruchaud
Format: Article
Language:English
Published: Taylor & Francis Group 2020-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
imidazopyridazine
haspin kinase
co-crystallisation and docking
cellular effects
3d spheroids
Online Access:http://dx.doi.org/10.1080/14756366.2020.1825408

Internet

http://dx.doi.org/10.1080/14756366.2020.1825408

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