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

IF 6.8 1区医学 Q1 CHEMISTRY, MEDICINAL

Journal of Medicinal Chemistry Pub Date : 2022-03-02 DOI:10.1021/acs.jmedchem.1c01654

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

引用次数: 2

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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靶向剪接体的水溶性异黄酮-磷酸类似物体内抗肿瘤活性的生物学研究

本文首次合成了天然产物异ginginggetin以及四种水溶性异ginginggetin -phosphate类似物。此外，本文还公开了IP2磷酸类似物在药理学特性(代谢和血浆稳定性、药代动力学、脱靶等)以及体外和体内生物活性方面的全面研究。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Medicinal Chemistry 医学-医药化学

CiteScore

4.00

自引率

11.00%

发文量

804

审稿时长

1.9 months

期刊介绍： The Journal of Medicinal Chemistry is a prestigious biweekly peer-reviewed publication that focuses on the multifaceted field of medicinal chemistry. Since its inception in 1959 as the Journal of Medicinal and Pharmaceutical Chemistry, it has evolved to become a cornerstone in the dissemination of research findings related to the design, synthesis, and development of therapeutic agents. The Journal of Medicinal Chemistry is recognized for its significant impact in the scientific community, as evidenced by its 2022 impact factor of 7.3. This metric reflects the journal's influence and the importance of its content in shaping the future of drug discovery and development. The journal serves as a vital resource for chemists, pharmacologists, and other researchers interested in the molecular mechanisms of drug action and the optimization of therapeutic compounds.