title: Aryl-acetic and cinnamic acids as lipoxygenase inhibitors with antioxidant, anti-inflammatory, and anticancer activity.
abstract: Cinnamic acids have been identified as interesting compounds with cytotoxic, anti-inflammatory, and antioxidant properties. Lipoxygenase pathway, catalyzing the first two steps of the transformation of arachidonic acid into leukotrienes is implicated in several processes such as cell differentiation, inflammation and carcinogenesis. Development of drugs that interfere with the formation or effects of these metabolites would be important for the treatment of various diseases like asthma, psoriasis, ulcerative colitis, rheumatoid arthritis, atherosclerosis, cancer, and blood vessel disorders. Till now, asthma consists of the only pathological case in which improvement has been shown by lipoxygenase LO inhibitors. Thus, the research has been directed towards the development of drugs that interfere with the formation of leukotrienes. In order to explore the anti-inflammatory and cytotoxic effects of antioxidant acrylic/cinnamic acids a series of derivatives bearing the appropriate moieties have been synthesized via the Knoevenagel condensation and evaluated for their biological activities. The compounds have shown important antioxidant activity, anti-inflammatory activity and very good inhibition of soybean lipoxygenase while some of them were tested for their anticancer activity.
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, University Campus, Thessaloniki, 54124, Greece, hadjipav@pharm.auth.gr.
authors.forename: Dimitra
authors.initials: D
authors.lastname: Hadjipavlou-Litina
authors.forename: Eleni
authors.initials: E
authors.lastname: Pontiki
mesh_terms: D019342:Acetic Acid / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000627:therapeutic use; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D000975:Antioxidants / Q000494:pharmacology* / Q000627:therapeutic use; D016718:Arachidonic Acid / Q000378:metabolism; D001713:Biphenyl Compounds / Q000737:chemistry; D045744:Cell Line, Tumor; D002934:Cinnamates / Q000494:pharmacology* / Q000627:therapeutic use; D051545:Cyclooxygenase 1 / Q000378:metabolism; D004487:Edema / Q000188:drug therapy / Q000473:pathology; D016166:Free Radical Scavengers / Q000494:pharmacology; D006418:Heme / Q000737:chemistry; D006801:Humans; D017665:Hydroxyl Radical / Q000737:chemistry; D015227:Lipid Peroxidation / Q000187:drug effects; D008084:Lipoxygenase / Q000378:metabolism; D016859:Lipoxygenase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D010851:Picrates / Q000737:chemistry; D051381:Rats; D013025:Glycine max / Q000201:enzymology
chemical_list: D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D000975:Antioxidants; D001713:Biphenyl Compounds; D002934:Cinnamates; D016166:Free Radical Scavengers; D016859:Lipoxygenase Inhibitors; D010851:Picrates; C029010:cinnamic acid; D016718:Arachidonic Acid; D017665:Hydroxyl Radical; D006418:Heme; C004931:1,1-diphenyl-2-picrylhydrazyl; D008084:Lipoxygenase; D051545:Cyclooxygenase 1; D019342:Acetic Acid