Steering target selectivity and potency by fragment-based de novo drug design.

Angew Chem Int Ed Engl

Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Zürich, Wolfgang-Pauli-Str. 10, 8093 Zürich (Switzerland).

Published: September 2013

Kinase inhibitors: Ligand-based de novo design is validated as a viable technology for rapidly generating innovative compounds possessing the desired biochemical profile. The study discloses the discovery of the most selective vascular endothelial growth factor receptor-2 (VEGFR-2) kinase inhibitor (right in scheme) known to date as prime lead for antiangiogenic drug development.

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Source
http://dx.doi.org/10.1002/anie.201304847DOI Listing

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