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

Tiago Rodrigues; Takayuki Kudoh; Filip Roudnicky; Yi Fan Lim; Yen Chu Lin; Christian P. Koch; Masaharu Seno; Michael Detmar; Gisbert Schneider

doi:10.1002/anie.201304847

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

Tiago Rodrigues, Takayuki Kudoh, Filip Roudnicky, Yi Fan Lim, Yen Chu Lin, Christian P. Koch, Masaharu Seno, Michael Detmar, Gisbert Schneider

Research output: Contribution to journal › Article › peer-review

21 Citations (Scopus)

Abstract

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.

Original language	English
Pages (from-to)	10006-10009
Number of pages	4
Journal	Angewandte Chemie - International Edition
Volume	52
Issue number	38
DOIs	https://doi.org/10.1002/anie.201304847
Publication status	Published - Sept 16 2013

Keywords

VEGFR
drug design
drug discovery
fragment-based design
kinase inhibitors

ASJC Scopus subject areas

Catalysis
Chemistry(all)

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10.1002/anie.201304847

Cite this

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AU - Rodrigues, Tiago

AU - Kudoh, Takayuki

AU - Roudnicky, Filip

AU - Lim, Yi Fan

AU - Lin, Yen Chu

AU - Koch, Christian P.

AU - Seno, Masaharu

AU - Detmar, Michael

AU - Schneider, Gisbert

PY - 2013/9/16

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KW - drug design

KW - drug discovery

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KW - kinase inhibitors

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

Abstract

Keywords

ASJC Scopus subject areas

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