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探索基于香豆素的衍生物作为生物活性分子的二十年历程。

A twenty-year journey exploring coumarin-based derivatives as bioactive molecules.

作者信息

Pisani Leonardo, Catto Marco, Muncipinto Giovanni, Nicolotti Orazio, Carrieri Antonio, Rullo Mariagrazia, Stefanachi Angela, Leonetti Francesco, Altomare Cosimo

机构信息

Department of Pharmacy-Pharmaceutical Sciences, University of Bari Aldo Moro, Bari, Italy.

Photys Therapeutics, Cambridge, MA, United States.

出版信息

Front Chem. 2022 Oct 10;10:1002547. doi: 10.3389/fchem.2022.1002547. eCollection 2022.

Abstract

The coumarin core (i.e., 1-benzopyran-2 (2)-one) is a structural motif highly recurrent in both natural products and bioactive molecules. Indeed, depending on the substituents and branching positions around the byciclic core, coumarin-containing compounds have shown diverse pharmacological activities, ranging from anticoagulant activities to anti-inflammatory, antimicrobial, anti-HIV and antitumor effects. In this survey, we have reported the main scientific results of the 20-years investigation on the coumarin core, exploited by the research group headed by Prof. Angelo Carotti (Bari, Italy) either as a scaffold or a pharmacophore moiety in designing novel biologically active small molecules.

摘要

香豆素核心结构(即1-苯并吡喃-2(2H)-酮)是天然产物和生物活性分子中高度常见的结构基序。实际上,根据双环核心周围的取代基和分支位置,含香豆素的化合物已显示出多种药理活性,从抗凝血活性到抗炎、抗菌、抗HIV和抗肿瘤作用。在本次综述中,我们报告了由安杰洛·卡罗蒂教授(意大利巴里)领导的研究小组对香豆素核心进行的20年研究的主要科学成果,该研究将香豆素核心作为设计新型生物活性小分子的支架或药效团部分进行了探索。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0656/9590106/34d986a8424b/fchem-10-1002547-g001.jpg

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