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

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

  • J Med Chem. 2022 Mar 24;65(6):4633-4648. doi: 10.1021/acs.jmedchem.1c01654.
Boris Letribot 1,  Megane Nascimento 2,  Giulia Cerrato 3,  Romain Darrigrand 2,  Valerie Salgues 2,  Dolor Renko 1,  Alain Pruvost 4,  Mouad Alami 1,  Samir Messaoudi 1,  Sebastien Apcher 2
Affiliations

Affiliations

  • 1 Université Paris-Saclay, CNRS, BioCIS, Châtenay-Malabry 92290, France.
  • 2 Université Paris-Saclay, Institut Gustave Roussy, Inserm, Immunologie des tumeurs et Immunothérapie, Villejuif 94805, France.
  • 3 Université Paris-Saclay, Institut Gustave Roussy, Metabolomics and Cell Biology Platforms, Villejuif 94805, France.
  • 4 Université Paris-Saclay, CEA, INRAE, Département Médicaments et Technologies pour La Santé, SPI, Gif-sur-Yvette 91191, France.
PMID: 35235336 DOI: 10.1021/acs.jmedchem.1c01654
Abstract

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.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-144655
    免疫调节剂
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