Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors
Graphical abstract
Starting from quinazoline 3a, we identified 3d a potent and selective ALK5 inhibitor over p38MAP kinase suitable for oral administration.
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Acknowledgements
We acknowledge Géraldine Poulain and Christelle Sury-Martin for their contribution to the synthesis of these compounds, and the DMPK team for performing the pharmacokinetic study.
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