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

doi:10.1021/acs.jmedchem.1c01654

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

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	4633-4648
Number of pages	16
Journal	Journal of Medicinal Chemistry
Volume	65
Issue number	6
DOIs	https://doi.org/10.1021/acs.jmedchem.1c01654
Publication status	Published - 24 Mar 2022
Externally published	Yes

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10.1021/acs.jmedchem.1c01654

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Letribot, B., Nascimento, M., Cerrato, G., Darrigrand, R., Salgues, V., Renko, D., Pruvost, A., Alami, M., Messaoudi, S., & Apcher, S. (2022). Biological Investigation of a Water-Soluble Isoginkgetin-Phosphate Analogue, Targeting the Spliceosome with In Vivo Antitumor Activity. Journal of Medicinal Chemistry, 65(6), 4633-4648. https://doi.org/10.1021/acs.jmedchem.1c01654

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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.",

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Letribot, B, Nascimento, M, Cerrato, G, Darrigrand, R, Salgues, V, Renko, D, Pruvost, A, Alami, M, Messaoudi, S & Apcher, S 2022, 'Biological Investigation of a Water-Soluble Isoginkgetin-Phosphate Analogue, Targeting the Spliceosome with In Vivo Antitumor Activity', Journal of Medicinal Chemistry, vol. 65, no. 6, pp. 4633-4648. https://doi.org/10.1021/acs.jmedchem.1c01654

TY - JOUR

T1 - Biological Investigation of a Water-Soluble Isoginkgetin-Phosphate Analogue, Targeting the Spliceosome with In Vivo Antitumor Activity

AU - Letribot, Boris

AU - Nascimento, Megane

AU - Cerrato, Giulia

AU - Darrigrand, Romain

AU - Salgues, Valerie

AU - Renko, Dolor

AU - Pruvost, Alain

AU - Alami, Mouad

AU - Messaoudi, Samir

AU - Apcher, Sebastien

PY - 2022/3/24

Y1 - 2022/3/24

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AB - 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.

UR - https://www.scopus.com/pages/publications/85126366432

U2 - 10.1021/acs.jmedchem.1c01654

DO - 10.1021/acs.jmedchem.1c01654

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ER -

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

Abstract

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