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 ApcherPublished 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.