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选择性 COX-2 抑制剂作为抗癌药物:专利审查(2014-2018 年)。

Selective COX-2 inhibitors as anticancer agents: a patent review (2014-2018).

机构信息

a Department of Medicinal Chemistry, School of Pharmacy , Shahid Beheshti University of Medical Sciences , Tehran , Iran.

出版信息

Expert Opin Ther Pat. 2019 Jun;29(6):407-427. doi: 10.1080/13543776.2019.1623880. Epub 2019 May 27.

Abstract

INTRODUCTION

COX-2 is a key enzyme in the process of prostaglandins (PGs) synthesis. The products of this enzyme could play a major role as the mediators of the inflammatory response and some other medical states such as cancer. The design and synthesis of novel selective COX-2 inhibitors have always been attractive to researchers. This review discusses the structures of novel COX-2 inhibitors synthesized during the last five years and describes their efficacy as anticancer agents.

AREAS COVERED

It is well established that COX-2 is overexpressed in many different cancers and treatment with selective COX-2 inhibitors could relieve their symptoms and limit their adverse sequences.

EXPERT OPINION

The diversity of selective COX-2 inhibitors is mainly related to the types of scaffolds. Monocyclic, bicyclic, tricyclic, and acyclic scaffolds with different pharmacological effects and toxicological profiles could be found in the family of selective COX-2 inhibitors. The great interest of the researchers in this field is due to the importance of selective COX-2 inhibitors as a relatively safe and effective set of compounds which could present different properties such as antirheumatic, anti-inflammatory, antiplatelet, anti-Alzheimer's disease, anti-Parkinson's disease, and anticancer.

摘要

简介

COX-2 是前列腺素(PGs)合成过程中的关键酶。该酶的产物可能作为炎症反应和其他一些医学状态(如癌症)的介质发挥主要作用。设计和合成新型选择性 COX-2 抑制剂一直吸引着研究人员。本文综述了过去五年合成的新型 COX-2 抑制剂的结构,并描述了它们作为抗癌剂的疗效。

涵盖领域

众所周知,COX-2 在许多不同的癌症中过度表达,使用选择性 COX-2 抑制剂可以缓解其症状并限制其不良后果。

专家意见

选择性 COX-2 抑制剂的多样性主要与支架类型有关。在选择性 COX-2 抑制剂家族中,可以发现具有不同药理作用和毒理学特征的单环、双环、三环和无环支架。研究人员对该领域的极大兴趣归因于选择性 COX-2 抑制剂作为一组相对安全有效的化合物的重要性,这些化合物可能具有不同的特性,如抗风湿、抗炎、抗血小板、抗阿尔茨海默病、抗帕金森病和抗癌。

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