title: Hypoxia-inducible factor inhibitors: a survey of recent patented compounds (2004 - 2010).
abstract: BACKGROUND
  Hypoxia-inducible factor (HIF) is a heterodimeric transcription factor consisting of α and β subunits that regulates the expression of angiogenic factors, including VEGF, which are involved in angiogenesis, invasion/metastasis, glucose uptake and cell survival during cancer development.
  
  
  METHODS
  This review summarizes the information about patented HIF inhibitors over the last 7 years (2004 - 2010). The reader will gain an outline of the structure and biological activity of recently developed HIF inhibitors.
  
  
  CONCLUSIONS
  Inhibition of HIF is an attractive therapeutic target for tumor angiogenesis and, until now, various HIF inhibitors have been discovered and evaluated. It is expected that development of more potent and selective HIF inhibitors will provide an effective treatment of cancer and other HIF-related diseases, including inflammation and cardiovascular disorder. As VEGF plays an important role in angiogenesis during tumor growth and ischemic diseases, the inhibition of VEGF-induced HIF is an attractive approach for the suppression of hypoxia-mediated pathological angiogenesis. HIF inhibitors may not only have cytostatic antitumor effects with fewer side effects, but also synergetic effects combined with radiotherapy.
authors.affiliation: Gakushuin University, Department of Chemistry, Faculty of Science, 1-5-1, Mejiro, Toshima-ku, Tokyo, 171-8588, Japan.
authors.forename: Hyun Seung
authors.initials: HS
authors.lastname: Ban
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Uto
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Nakamura
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D004220:Disulfides / Q000494:pharmacology / Q000627:therapeutic use; D004958:Estradiol / Q000031:analogs & derivatives / Q000494:pharmacology; D005663:Furans / Q000494:pharmacology; D006801:Humans; D051795:Hypoxia-Inducible Factor 1, alpha Subunit / Q000037:antagonists & inhibitors*; D007093:Imidazoles / Q000494:pharmacology / Q000627:therapeutic use; D007191:Indazoles / Q000494:pharmacology; D009150:Mustard Compounds / Q000494:pharmacology / Q000627:therapeutic use; D010330:Patents as Topic; D010666:Phenylpropionates / Q000494:pharmacology / Q000627:therapeutic use; D010879:Piperazines / Q000494:pharmacology
chemical_list: C492908:2-amino-3-(4'-N,N-bis(2-chloroethyl)amino)phenylpropionic acid N-oxide; C551406:21-(2-(N,N-dimethylamino)ethyl)oxy-7a-methyl-19-norpregna-1,3,5(10),17(20)-tetraen-3-ol; D000970:Antineoplastic Agents; D004220:Disulfides; D005663:Furans; D051795:Hypoxia-Inducible Factor 1, alpha Subunit; D007093:Imidazoles; D007191:Indazoles; D009150:Mustard Compounds; D010666:Phenylpropionates; D010879:Piperazines; C482885:manassantin B; C090937:3-(5'-hydroxymethyl-2'-furyl)-1-benzylindazole; C002511:chaetocin; D004958:Estradiol; C412893:1-methylpropyl-2-imidazolyl disulfide