title: Vitamin E derivatives: a patent review (2010 - 2015).
abstract: BACKGROUND
  The vitamin E family consists of four tocopherols and four tocotrienols. α-Tocopherol is the most studied member of this family for its antioxidant and non-antioxidant properties, while tocotrienols have attracted recent research interest. The structural motifs of the vitamin E family and specifically the chroman moiety, are amenable to various modifications in order to improve their bioactivities towards numerous therapeutic targets.
  
  
  METHODS
  This review includes the patent literature from 2010 - 2015 related to vitamin E derivatives and it is focused on 2-, 5- or 6-substituted chroman analogues. The patent search was performed using Reaxys® and esp@cenet.
  
  
  CONCLUSIONS
  The chroman moiety of vitamin E is a privileged structure and an essential pharmacophore which inspired organic chemists to synthesize new analogues with improved bioactivities. Modifications at the 2- and 5- positions of the chroman ring resulted in very interesting active compounds in cellular and animal models of diseases related to oxidative stress. More recent publications and patents reported 6-substituted chromans as anticancer agents in vitro and in vivo. Additionally, an emerging interest is observed towards the use of vitamin E analogues incorporated in drug delivery systems and for medical imaging as contrast agents or fluorescent probes.
authors.affiliation: a Research Director, Institute of Biology, Medicinal Chemistry and Biotechnology , National Hellenic Research Foundation , 11635 Athens , Greece.
authors.forename: Maria
authors.initials: M
authors.lastname: Koufaki
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D000975:Antioxidants / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D018384:Oxidative Stress / Q000187:drug effects; D010330:Patents as Topic; D024505:Tocopherols / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D024508:Tocotrienols / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D024508:Tocotrienols; D024505:Tocopherols
keywords: anticancer; antioxidant; chroman; drug delivery; vitamin E