Chalcones as Potential Cyclooxygenase-2 Inhibitors: A Review

被引:5
作者
Mahboubi-Rabbani, Mohammad [1 ]
Zarei, Rosa [1 ]
Baradaran, Mehdi [1 ]
Bayanati, Maryam [2 ]
Zarghi, Afshin [3 ]
机构
[1] Islamic Azad Univ, Sch Pharm, Dept Med Chem, Tehran, Iran
[2] Shahid Beheshti Univ Med Sci, Natl Nutr & Food Technol Res Inst, Fac Nutr Sci & Food Technol, Dept Food Technol Res, Tehran, Iran
[3] Shahid Beheshti Univ Med Sci, Sch Pharm, Dept Med Chem, Tehran, Iran
关键词
Chalcones; COX-2; inhibitors; prostaglandins; inflammation; cancer; neurodegenerative diseases; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; PROLIFERATOR-ACTIVATED RECEPTORS; BIOLOGICAL EVALUATION; AGENTS DESIGN; ANTICANCER AGENTS; COX-2; INHIBITORS; CANCER; DERIVATIVES; EXPRESSION; CHALLENGES;
D O I
10.2174/0118715206267309231103053808
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
Cyclooxygenases (COXs) play a pivotal role in inflammation, a complex phenomenon required in human defense, but also involved in the emergence of insidious human disorders. Currently-used COX-1 inhibitors (Non-Steroidal Anti-Inflammatory Drugs-NSAIDs), as the most frequent choices for the treatment of chronic inflammatory diseases, have been identified to be associated with a variety of adverse drug reactions, especially dyspepsia, as well as peptic ulcer, which lead to diminished output. Moreover, the structural similarities of COX-1 and -2, along with the availability of comprehensive information about the three-dimensional structure of COX-2, co-crystallized with various inhibitors, search selective COX-2 inhibitors a formidable challenge. COX-2 inhibitors were shown to minimize the incidence of metastasis in cancer patients when administered preoperatively. Developing selective COX-2 inhibitors to tackle both cancer and chronic inflammatory illnesses has been identified as a promising research direction in recent decades. Identifying innovative scaffolds to integrate as the major component of future COX-2 inhibitors is critical in this regard. The presence of a central, alpha, beta-unsaturated carbonyl-containing scaffold, as a characteristic structural pattern in many selective COX-2 inhibitors, along with a huge count of chalcone-based anticancer agents representing the basic idea of this review; providing a survey of the most recently published literature concerning development of chalcone analogs as novel COX-2 inhibitors until 2022 with efficient anticancer activity. A brief overview of the most recent developments concerning structure-activity relationship insights and mechanisms is also reported, helping pave the road for additional investigation.
引用
收藏
页码:77 / 95
页数:19
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