title: Cyclooxygenase-2 inhibitors: a literature and patent review (2009 - 2010).
abstract: BACKGROUND
  COXs catalyze the complex conversion of arachidonic acid to prostaglandins and thromboxanes, which trigger as autacoids with autocrine and paracrine biological effects many physiological and pathophysiological responses. The structural similarities of the COX-1 and -2 enzymes make the search for selective inhibitors for COX-2 versus -1 a formidable challenge.
  
  
  METHODS
  The present review provides a survey of the development of novel COX-2 inhibitors covering literature and patents between 2009 and 2010. The presence of a central, typically 1,2-diaryl substituted, heterocycle or carbocycle as a characteristic structural motif in many selective COX-2 inhibitors represents the basis of their classification in this review. The classification in this review includes COX-2 inhibitors based on five- and six-membered heterocycles, benzoheterocycles (e.g., benzopyrans, benzopyranones, indoles and quinolines), quinones, chalcones, natural products and miscellaneous. When available, COX-2 inhibitors are presented with their related COX-2 inhibitory potency and selectivity.
  
  
  CONCLUSIONS
  The availability of detailed information on the crystal structure of the COX-2 enzyme with various substrates, cofactors and inhibitors, and the recently reported increased risk of cardiovascular events associated with selective COX-2 inhibitors will further stimulate development of COX-2 inhibitors with favorable COX-2 inhibition profiles without adverse effects to the cardiovascular system.
authors.affiliation: University of Alberta, Department of Oncology , Edmonton , Canada.
authors.forename: Baker
authors.initials: B
authors.lastname: Jawabrah Al-Hourani
authors.forename: Sai Kiran
authors.initials: SK
authors.lastname: Sharma
authors.forename: Mavanur
authors.initials: M
authors.lastname: Suresh
authors.forename: Frank
authors.initials: F
authors.lastname: Wuest
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000494:pharmacology; D001688:Biological Products / Q000494:pharmacology; D051545:Cyclooxygenase 1 / Q000378:metabolism; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D051379:Mice; D010330:Patents as Topic; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D001688:Biological Products; D052246:Cyclooxygenase 2 Inhibitors; D016861:Cyclooxygenase Inhibitors; D006571:Heterocyclic Compounds; D051545:Cyclooxygenase 1