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塞来昔布类似物作为抗癌药物研发的最新进展:综述

Recent advances in the development of celecoxib analogs as anticancer agents: A review.

作者信息

Abdelhaleem Eman F, Kassab Asmaa E, El-Nassan Hala B, Khalil Omneya M

机构信息

Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo, Egypt.

出版信息

Arch Pharm (Weinheim). 2022 Dec;355(12):e2200326. doi: 10.1002/ardp.202200326. Epub 2022 Aug 22.

Abstract

Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) designed to be a selective cyclooxygenase-2 (COX-2) inhibitor. It was approved by the U.S. Food and Drug Administration for the treatment of inflammatory diseases such as osteoarthritis and rheumatoid arthritis. Additionally, celecoxib demonstrated potent antitumor and chemopreventive effects in vitro, in vivo, and in patients. The mechanism of celecoxib's chemopreventive effect is still not fully identified, but it is assumed to be multifactorial. Celecoxib's anticancer activity has been described both as independent of and dependent on its COX-2 inhibitory activity. The current review summarizes the recent advances published between 2000 and 2022 on the structure-based optimization of celecoxib to develop compounds with promising anticancer activity. The structure-activity relationships of celecoxib analogs are discussed, which may be beneficial in the design and development of novel analogs as potent antiproliferative agents in the future.

摘要

塞来昔布是一种非甾体抗炎药(NSAID),设计为选择性环氧化酶-2(COX-2)抑制剂。它被美国食品药品监督管理局批准用于治疗骨关节炎和类风湿关节炎等炎症性疾病。此外,塞来昔布在体外、体内和患者中均显示出强大的抗肿瘤和化学预防作用。塞来昔布化学预防作用的机制仍未完全明确,但推测是多因素的。塞来昔布的抗癌活性既有独立于其COX-2抑制活性的描述,也有依赖于该活性的描述。本综述总结了2000年至2022年间发表的关于基于结构优化塞来昔布以开发具有潜在抗癌活性化合物的最新进展。讨论了塞来昔布类似物的构效关系,这可能有助于未来设计和开发新型类似物作为有效的抗增殖剂。

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