Nimesulide analogues: From anti-inflammatory to antitumor agents

• Published in: Bioorganic chemistry Vol. 88; p. 102966
• Main Authors: Catarro, Mafalda, Serrano, João L., Ramos, Susana S., Silvestre, Samuel, Almeida, Paulo
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.07.2019
• Subjects: Anti-inflammatory activity; Antitumor activity; Cyclooxygenase-2 inhibition; Nimesulide analogues; Synthetic approaches; Ac; FDA; SRB; COX-2; PGH2; COX-1; COX-3; LTEDaro; TMPD; MTT; Synthetic approaches; LPS; Et; Ar; THF; Cy; NSAIDs; IC50; DMAP; Ph; ED50; DMF; PGE2; Pr; USA; Cyclooxygenase-2 inhibition; EDCI; Nimesulide analogues; PGG2; Py; IPr; Bn; COX; HetAr; Bu; Me; Anti-inflammatory activity; Antitumor activity; Hex
• ISSN: 0045-2068; 1090-2120
• DOI: 10.1016/j.bioorg.2019.102966

[Display omitted] •Nimesulide is an anti-inflammatory drug recently associated to antitumor activity.•The synthesis approaches for nimesulide derivatives is in special described.•Their biological activity from anti-inflammatory to antitumor is also described. Nimesulide is a nonsteroidal anti-inflammatory drug possessing analgesic and antipyretic properties. This drug is considered a selective cyclooxygenase-2 (COX-2) inhibitor and, more recently, has been associated to antitumor activity. Thus, numerous works have been developed to modify the nimesulide skeleton aiming to develop new and more potent and selective COX-2 inhibitors as well as potential anticancer agents. This review intends to provide an overview on analogues of nimesulide, including the general synthetic approaches used for their preparation and structural diversification and their main anti-inflammatory and/or antitumor properties.