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

机译:选择性Cox-2抑制剂作为抗癌剂:专利审查(2014-2018)

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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.
机译:简介:COX-2是前列腺素(PGS)合成过程中的关键酶。这种酶的产品可以作为炎症反应的介质和癌症如癌症的其他一些医学态起到重要作用。新型选择性COX-2抑制剂的设计和合成对研究人员来说一直是有吸引力的。本综述讨论了在过去五年中合成的新型COX-2抑制剂的结构,并将其疗效描述为抗癌剂。覆盖:很好地确定,COX-2在许多不同的癌症中过表达和用选择性COX-2抑制剂治疗可以缓解它们的症状并限制其不利序列。普及意见:选择性Cox-2抑制剂的多样性主要与支架的类型有关。在选择性Cox-2抑制剂的家族中可以发现单环,双环,三环和无环支架,具有不同的药理作用和毒理学曲线。该领域的研究人员的巨大兴趣是由于选择性Cox-2抑制剂作为相对安全有效的化合物的重要性,这可能呈现不同性质,例如抗炎,抗炎,抗血小板,抗阿尔茨海默病,抗-Parkinson的疾病和抗癌。

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