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10.3390/biom11071049

http://scihub22266oqcxt.onion/10.3390/biom11071049
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34356673!8302000!34356673
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suck abstract from ncbi


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pmid34356673      Biomolecules 2021 ; 11 (7): ä
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  • Celecoxib Analogues for Cancer Treatment: An Update on OSU-03012 and 2,5-Dimethyl-Celecoxib #MMPMID34356673
  • Sobolewski C; Legrand N
  • Biomolecules 2021[Jul]; 11 (7): ä PMID34356673show ga
  • Cyclooxygenase-2 (COX-2) is an important enzyme involved in prostaglandins biosynthesis from arachidonic acid. COX-2 is frequently overexpressed in human cancers and plays a major tumor promoting function. Accordingly, many efforts have been devoted to efficiently target the catalytic site of this enzyme in cancer cells, by using COX-2 specific inhibitors such as celecoxib. However, despite their potent anti-tumor properties, the myriad of detrimental effects associated to the chronic inhibition of COX-2 in healthy tissues, has considerably limited their use in clinic. In addition, increasing evidence indicate that these anti-cancerous properties are not strictly dependent on the inhibition of the catalytic site. These findings have led to the development of non-active COX-2 inhibitors analogues aiming at preserving the antitumor effects of COX-2 inhibitors without their side effects. Among them, two celecoxib derivatives, 2,5-Dimethyl-Celecoxib and OSU-03012, have been developed and suggested for the treatment of viral (e.g., recently SARS-CoV-2), inflammatory, metabolic diseases and cancers. These molecules display stronger anti-tumor properties than celecoxib and thus may represent promising anti-cancer molecules. In this review, we discuss the impact of these two analogues on cancerous processes but also their potential for cancer treatment alone or in combination with existing approaches.
  • |Animals[MESH]
  • |Antineoplastic Agents/adverse effects/chemistry/pharmacology/*therapeutic use[MESH]
  • |Celecoxib/adverse effects/analogs & derivatives/pharmacology/*therapeutic use[MESH]
  • |Cell Cycle/drug effects[MESH]
  • |Cyclooxygenase 2 Inhibitors/adverse effects/chemistry/pharmacology/*therapeutic use[MESH]
  • |Humans[MESH]
  • |Neoplasms/*drug therapy[MESH]
  • |Pyrazoles/adverse effects/chemistry/pharmacology/*therapeutic use[MESH]


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