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Biological Investigation of a Water-Soluble Isoginkgetin-Phosphate Analogue, Targeting the Spliceosome with In Vivo Antitumor Activity.
Letribot, Boris; Nascimento, Megane; Cerrato, Giulia; Darrigrand, Romain; Salgues, Valerie; Renko, Dolor; Pruvost, Alain; Alami, Mouad; Messaoudi, Samir; Apcher, Sebastien.
Afiliação
  • Letribot B; Université Paris-Saclay, CNRS, BioCIS, Châtenay-Malabry 92290, France.
  • Nascimento M; Université Paris-Saclay, Institut Gustave Roussy, Inserm, Immunologie des tumeurs et Immunothérapie, Villejuif 94805, France.
  • Cerrato G; Université Paris-Saclay, Institut Gustave Roussy, Metabolomics and Cell Biology Platforms, Villejuif 94805, France.
  • Darrigrand R; Université Paris-Saclay, Institut Gustave Roussy, Inserm, Immunologie des tumeurs et Immunothérapie, Villejuif 94805, France.
  • Salgues V; Université Paris-Saclay, Institut Gustave Roussy, Inserm, Immunologie des tumeurs et Immunothérapie, Villejuif 94805, France.
  • Renko D; Université Paris-Saclay, CNRS, BioCIS, Châtenay-Malabry 92290, France.
  • Pruvost A; Université Paris-Saclay, CEA, INRAE, Département Médicaments et Technologies pour La Santé, SPI, Gif-sur-Yvette 91191, France.
  • Alami M; Université Paris-Saclay, CNRS, BioCIS, Châtenay-Malabry 92290, France.
  • Messaoudi S; Université Paris-Saclay, CNRS, BioCIS, Châtenay-Malabry 92290, France.
  • Apcher S; Université Paris-Saclay, Institut Gustave Roussy, Inserm, Immunologie des tumeurs et Immunothérapie, Villejuif 94805, France.
J Med Chem ; 65(6): 4633-4648, 2022 03 24.
Article em En | MEDLINE | ID: mdl-35235336
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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Spliceossomos / Biflavonoides Idioma: En Ano de publicação: 2022 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Spliceossomos / Biflavonoides Idioma: En Ano de publicação: 2022 Tipo de documento: Article