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Coumarin sulfonamides derivatives as potent and selective COX-2 inhibitors with efficacy in suppressing cancer proliferation and metastasis.香豆素磺酰胺衍生物作为强效且选择性的COX-2抑制剂，在抑制癌症增殖和转移方面具有疗效。
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Rational Design of Small Peptides for Optimal Inhibition of Cyclooxygenase-2: Development of a Highly Effective Anti-Inflammatory Agent.合理设计小分子肽以实现环氧化酶-2 的最佳抑制：高效抗炎药物的研发。
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Low-dose Aspirin, Nonsteroidal Anti-inflammatory Drugs, Selective COX-2 Inhibitors and Breast Cancer Recurrence.低剂量阿司匹林、非甾体抗炎药、选择性环氧化酶-2抑制剂与乳腺癌复发
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COX-2 modulates mammary tumor progression in response to collagen density.COX-2 根据胶原蛋白密度调节乳腺肿瘤进展。
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Design and Synthesis of New Transient Receptor Potential Vanilloid Type-1 (TRPV1) Channel Modulators: Identification, Molecular Modeling Analysis, and Pharmacological Characterization of the N-(4-Hydroxy-3-methoxybenzyl)-4-(thiophen-2-yl)butanamide, a Small Molecule Endowed with Agonist TRPV1 Activity and Protective Effects against Oxidative Stress.新型瞬时受体电位香草酸型 1（TRPV1）通道调节剂的设计与合成：N-（4-羟基-3-甲氧基苄基）-4-（噻吩-2-基）丁酰胺的鉴定、分子建模分析和药理学特性研究，该小分子具有 TRPV1 激动剂活性和抗氧化应激保护作用。
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选择性环氧化酶2抑制剂合成的构效关系概述（2009 - 2016年）

Structure-activity relationships for the synthesis of selective cyclooxygenase 2 inhibitors: an overview (2009-2016).

作者信息

Carullo G, Galligano F, Aiello F

机构信息

Department of Pharmacy, Health and Nutritional Sciences , University of Calabria , 87036 Rende , Italy . Email:

出版信息

Medchemcomm. 2016 Dec 12;8(3):492-500. doi: 10.1039/c6md00569a. eCollection 2017 Mar 1.

DOI:10.1039/c6md00569a
PMID:30108767
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6072045/
Abstract

Most drugs used to treat pain and inflammation act through inhibition of the enzymes prostaglandin G/H synthase, commonly known as cyclooxygenase (COX). Among these, the simultaneous inhibition of cyclooxygenase 1 (COX-1) would explain the unwanted side effects in the gastrointestinal tract and many adverse cardiovascular effects, such as high blood pressure, myocardial infarction and thrombosis. These side effects led in time to the development of NSAIDs that behave as selective COX-2 inhibitors. This manuscript highlights the structure-activity relationships which characterize the chemical scaffolds endowed with selective COX-2 inhibition. Additionally, the role of COX-2 inhibitors in the pain phenomenon and cancer is discussed.

摘要

大多数用于治疗疼痛和炎症的药物通过抑制前列腺素G/H合酶（通常称为环氧化酶（COX））发挥作用。其中，同时抑制环氧化酶1（COX-1）会导致胃肠道出现不良副作用以及许多不良心血管效应，如高血压、心肌梗死和血栓形成。这些副作用促使了非甾体抗炎药（NSAIDs）的发展，这类药物表现为选择性COX-2抑制剂。本手稿重点介绍了具有选择性COX-2抑制作用的化学支架所具有的构效关系。此外，还讨论了COX-2抑制剂在疼痛现象和癌症中的作用。