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

Boris Letribot,Megane Nascimento,Giulia Cerrato,Romain Darrigrand,Valerie Salgues,Dolor Renko,Alain Pruvost,Mouad Alami,Samir Messaoudi,Sebastien Apcher

JOURNAL OF MEDICINAL CHEMISTRY（2022）

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摘要

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 theIP2phosphate analogue with respectto pharmacological properties (metabolicandplasmaticstabilities, pharmacokinetic, off-target, etc.) as well as in vitro and in vivo biological activities are disclosed herein

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