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

• Main Authors: Jonathan Elie (Author), Omid Feizbakhsh (Author), Nathalie Desban (Author), Béatrice Josselin (Author), Blandine Baratte (Author), Amandine Bescond (Author), Julien Duez (Author), Xavier Fant (Author), Stéphane Bach (Author), Dominique Marie (Author), Matthieu Place (Author), Sami Ben Salah (Author), Agnes Chartier (Author), Sabine Berteina-Raboin (Author), Apirat Chaikuad (Author), Stefan Knapp (Author), Fabrice Carles (Author), Pascal Bonnet (Author), Frédéric Buron (Author), Sylvain Routier (Author), Sandrine Ruchaud (Author)
• Format: Book
• Published: Taylor & Francis Group, 2020-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...