title: Natural and synthetic α,β-unsaturated carbonyls for NF-κB inhibition.
abstract: BACKGROUND
  The nuclear transcription factor NF-κB has gained considerable importance due to its major involvement in inflammation and constitutive activity in malignant cells. It is induced by a variety of stimuli and controls the expression of several proteins involved in biological processes. Numerous natural products and synthesized organic molecules have been reported to inhibit NF-κB and have played an integral role in identifying implicated pathways. Prominent among them are the sesquiterpene lactones, polyphenolic enones and other α,β-unsaturated carbonyl-containing molecules, particularly α-methylene-γ-butyrolactones.
  
  
  CONCLUSIONS
  This mini-review provides an introductory overview of some of the associated pathways involving NF-κB in cancer and discusses the structures and mode of action of natural α,β-unsaturated carbonyl-containing inhibitors and their synthetic counterparts. A review of the recent methods for the synthesis of α-alkylidene-γ-butyrolactones is also provided, with the aim of arousing the interest of synthetic chemists for the design and development of novel NF-κB inhibitors.
  
  
  CONCLUSIONS
  Modulating damaging effects without harming the inflammatory and immune responses are crucial parameters for developing NF-κB inhibitors. Examination of novel α,β-unsaturated carbonyls and the further discovery of simple methods to prepare such molecules should lead to the identification of site-specific inhibitors.
authors.affiliation: Department of Chemistry, Purdue University, 560 Oval Drive, West Lafayette, IN 47907-2084, USA. chandran@purdue.edu
authors.forename: P Veeraraghavan
authors.initials: PV
authors.lastname: Ramachandran
authors.forename: Michele
authors.initials: M
authors.lastname: Yip-Schneider
authors.forename: C Max
authors.initials: CM
authors.lastname: Schmidt
mesh_terms: D002109:Caffeic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D016328:NF-kappa B / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011809:Quinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D012717:Sesquiterpenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013267:Stilbenes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D002109:Caffeic Acids; D005419:Flavonoids; D016328:NF-kappa B; D011809:Quinones; D012717:Sesquiterpenes; D013267:Stilbenes; C040048:caffeic acid