2012
M. Elagawany et al. / Bioorg. Med. Chem. Lett. 23 (2013) 2007–2013
Figure 7. Hypothetical binding mode of compound 20e in the active site of
DYRK1A.
Figure 9. 2D Interaction model of complex BRW-GSK3. Ligands BRW (red), 12
(green), and 13 (blue) are docked and shown with the residues of active site.
Hydrogen bonds are shown as dotted lines consistent with ligand colors.
References and notes
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Figure 8. 2D Interaction model of complex HRM-DYRK1A. Ligands HRM (pink), 20e
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In conclusion, we have designed and synthesized a new series of
bicyclic heteroaromatic systems of fused or linked types containing
pyridazinone fragment. Structure–activity relationships of these
compounds and cellular activities have been explored. Different
activity patterns were identified and investigated for three of these
inhibitors and kinases DYRK1A and GSK3. Dual and single kinases
inhibitors 13, 12, and 20e were identified and will be used as start-
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Authors are thankful to Dr. Jean Jacques Bourguignon, Dr. Martine
Schmitt, Dr. Frédéric Bihel, Dr. Laurent Meijer, Dr. Cláudia Pessoa
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Supplementary data
Supplementary data associated with this article can be found,
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