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 journalArticle

18 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 languageEnglish
Pages (from-to)10006-10009
Number of pages4
JournalAngewandte Chemie - International Edition
Volume52
Issue number38
DOIs
Publication statusPublished - Sep 16 2013

Keywords

  • VEGFR
  • drug design
  • drug discovery
  • fragment-based design
  • kinase inhibitors

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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  • Cite this

    Rodrigues, T., Kudoh, T., Roudnicky, F., Lim, Y. F., Lin, Y. C., Koch, C. P., Seno, M., Detmar, M., & Schneider, G. (2013). Steering target selectivity and potency by fragment-based de novo drug design. Angewandte Chemie - International Edition, 52(38), 10006-10009. https://doi.org/10.1002/anie.201304847