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尼美舒利类似物:从抗炎剂到抗肿瘤剂。

Nimesulide analogues: From anti-inflammatory to antitumor agents.

机构信息

CICS-UBI - Health Sciences Research Center, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal.

FibEnTech - UBI, Materiais Fibrosos e Tecnologias Ambientais, University of Beira Interior, Rua Marquês d'Ávila e Bolama, 6200-001 Covilhã, Portugal.

出版信息

Bioorg Chem. 2019 Jul;88:102966. doi: 10.1016/j.bioorg.2019.102966. Epub 2019 Apr 30.

DOI:10.1016/j.bioorg.2019.102966
PMID:31075744
Abstract

Nimesulide is a nonsteroidal anti-inflammatory drug possessing analgesic and antipyretic properties. This drug is considered a selective cyclooxygenase-2 (COX-2) inhibitor and, more recently, has been associated to antitumor activity. Thus, numerous works have been developed to modify the nimesulide skeleton aiming to develop new and more potent and selective COX-2 inhibitors as well as potential anticancer agents. This review intends to provide an overview on analogues of nimesulide, including the general synthetic approaches used for their preparation and structural diversification and their main anti-inflammatory and/or antitumor properties.

摘要

尼美舒利是一种具有镇痛和解热作用的非甾体抗炎药。该药物被认为是一种选择性环氧化酶-2(COX-2)抑制剂,最近还与抗肿瘤活性相关。因此,已经开发了许多工作来修饰尼美舒利骨架,旨在开发新的、更有效和选择性的 COX-2 抑制剂以及潜在的抗癌药物。本文综述了尼美舒利类似物,包括用于其制备和结构多样化的一般合成方法及其主要的抗炎和/或抗肿瘤特性。

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