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Biological Investigation of a Water-Soluble Isoginkgetin-Phosphate Analogue, Targeting the Spliceosome with In Vivo Antitumor Activity.

Boris LetribotMegane NascimentoGiulia CerratoRomain DarrigrandValerie SalguesDolor RenkoAlain PruvostMouad AlamiSamir MessaoudiSebastien Apcher
Published in: Journal of medicinal chemistry (2022)
The first total synthesis of the natural product Isoginkgetin as well as four water-soluble Isoginkgetin-phosphate analogues is reported herein. Moreover, the full study of the IP2 phosphate analogue with respect to pharmacological properties (metabolic and plasmatic stabilities, pharmacokinetic, off-target, etc.) as well as in vitro and in vivo biological activities are disclosed herein.
Keyphrases
  • water soluble
  • molecular docking
  • structure activity relationship