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Design of granulatimide and isogranulatimide analogues as potential Chk1 inhibitors: Study of amino-platforms for their synthesis.

Abstract
The two marine alkaloids granulatimide and isogranulatimide have been shown to inhibit the checkpoint kinase 1 (Chk1), a promising target for cancer treatment. A molecular docking study allowing the design of new potential Chk1 inhibitors based on the natural products skeleton and the synthetic work to an amino-target platform to prepare them are described.
AuthorsHubert Lavrard, Frédéric Rodriguez, Evelyne Delfourne
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 22 Issue 17 Pg. 4961-7 (Sep 01 2014) ISSN: 1464-3391 [Electronic] England
PMID25047935 (Publication Type: Journal Article)
CopyrightCopyright © 2014 Elsevier Ltd. All rights reserved.
Chemical References
  • Alkaloids
  • Imidazoles
  • Indoles
  • Protein Kinase Inhibitors
  • granulatimide
  • isogranulatimide
  • Protein Kinases
  • Checkpoint Kinase 1
Topics
  • Alkaloids (chemical synthesis, chemistry, pharmacology)
  • Checkpoint Kinase 1
  • Dose-Response Relationship, Drug
  • Drug Design
  • Imidazoles (chemical synthesis, chemistry, pharmacology)
  • Indoles (chemical synthesis, chemistry, pharmacology)
  • Models, Molecular
  • Molecular Structure
  • Protein Kinase Inhibitors (chemical synthesis, chemistry, pharmacology)
  • Protein Kinases (metabolism)
  • Structure-Activity Relationship

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