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Chemical Compound Review

AC1O3S5O     (2Z,4R)-4-methyl-2-(3- oxopyridin-2...

Synonyms: 105635-69-6, Desferrithiocin
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Disease relevance of Desferrithiocin


High impact information on Desferrithiocin


Biological context of Desferrithiocin


Anatomical context of Desferrithiocin


Associations of Desferrithiocin with other chemical compounds


Analytical, diagnostic and therapeutic context of Desferrithiocin

  • This investigation thus demonstrates which structural components of the siderophore are required for iron clearance after oral administration and suggests the use of the desferrithiocin platform as a vector for other chelators [12].
  • Two protocols were investigated: "treated" recipients received desferrithiocin (30 mg/kg/day) orally for 10 days beginning the day of transplantation; "pretreated" hosts received a similar dose of the drug for 10 days before engraftment [13].
  • A subgroup of the orthosubstituted phenolate class of Fe chelators, desferrithiocin [2-(3'-hydroxypyrid-2'-yl)4-methyl-delta2-thiazoline-4(S)-carboxylic acid; DFT] and its analogues, have potential application in short-term chemotherapy for cancer by Fe deprivation [14].
  • The efficacy and toxicity of the siderophore desferrithiocin (DFT), which has shown potential application in iron chelation therapy, were assessed in vivo and in vitro [15].
  • Oral iron chelator desferrithiocin blocks allogeneic mononuclear cell activation and cytokine production in vivo and prolongs rat cardiac allograft survival [16].


  1. The effect of desferrithiocin, an oral iron chelator, on T-cell function. Bierer, B.E., Nathan, D.G. Blood (1990) [Pubmed]
  2. Effects of C-4 stereochemistry and C-4' hydroxylation on the iron clearing efficiency and toxicity of desferrithiocin analogues. Bergeron, R.J., Wiegand, J., McManis, J.S., McCosar, B.H., Weimar, W.R., Brittenham, G.M., Smith, R.E. J. Med. Chem. (1999) [Pubmed]
  3. Evaluation of desferrithiocin and its synthetic analogues as orally effective iron chelators. Bergeron, R.J., Wiegand, J., Dionis, J.B., Egli-Karmakka, M., Frei, J., Huxley-Tencer, A., Peter, H.H. J. Med. Chem. (1991) [Pubmed]
  4. Prevention of acetic acid-induced colitis by desferrithiocin analogs in a rat model. Bergeron, R.J., Wiegand, J., Weimar, W.R., Nguyen, J.N., Sninsky, C.A. Dig. Dis. Sci. (2003) [Pubmed]
  5. Role of oxidants in DNA damage. Hydroxyl radical mediates the synergistic DNA damaging effects of asbestos and cigarette smoke. Jackson, J.H., Schraufstatter, I.U., Hyslop, P.A., Vosbeck, K., Sauerheber, R., Weitzman, S.A., Cochrane, C.G. J. Clin. Invest. (1987) [Pubmed]
  6. A comparative study of the iron-clearing properties of desferrithiocin analogues with desferrioxamine B in a Cebus monkey model. Bergeron, R.J., Streiff, R.R., Creary, E.A., Daniels, R.D., King, W., Luchetta, G., Wiegand, J., Moerker, T., Peter, H.H. Blood (1993) [Pubmed]
  7. Desferrithiocin analogue based hexacoordinate iron(III) chelators. Bergeron, R.J., Huang, G., Weimar, W.R., Smith, R.E., Wiegand, J., McManis, J.S. J. Med. Chem. (2003) [Pubmed]
  8. Pharmacokinetics of orally administered desferrithiocin analogs in cebus apella primates. Bergeron, R.J., Weimar, W.R., Wiegand, J. Drug Metab. Dispos. (1999) [Pubmed]
  9. Iron chelators in cancer chemotherapy. Buss, J.L., Greene, B.T., Turner, J., Torti, F.M., Torti, S.V. Current topics in medicinal chemistry. (2004) [Pubmed]
  10. Iron chelators: in vitro inhibitory effect on the liver stage of rodent and human malaria. Stahel, E., Mazier, D., Guillouzo, A., Miltgen, F., Landau, I., Mellouk, S., Beaudoin, R.L., Langlois, P., Gentilini, M. Am. J. Trop. Med. Hyg. (1988) [Pubmed]
  11. Interference with oxidative processes inhibits proliferation of human peripheral blood lymphocytes and murine B-lymphocytes. Hunt, N.H., Cook, E.P., Fragonas, J.C. Int. J. Immunopharmacol. (1991) [Pubmed]
  12. The desferrithiocin pharmacophore. Bergeron, R.J., Liu, C.Z., McManis, J.S., Xia, M.X., Algee, S.E., Wiegand, J. J. Med. Chem. (1994) [Pubmed]
  13. Iron chelation suppresses mononuclear cell activation, modifies lymphocyte migration patterns, and prolongs rat cardiac allograft survival in rats. Whitley, W.D., Hancock, W.W., Kupiec-Weglinski, J.W., DeSousa, M., Tilney, N.L. Transplantation (1993) [Pubmed]
  14. The desferrithiocin (DFT) class of iron chelators: potential as antineoplastic agents. Kicic, A., Chua, A.C., Baker, E. Anticancer Drug Des. (2001) [Pubmed]
  15. Desferrithiocin is an effective iron chelator in vivo and in vitro but ferrithiocin is toxic. Baker, E., Wong, A., Peter, H., Jacobs, A. Br. J. Haematol. (1992) [Pubmed]
  16. Oral iron chelator desferrithiocin blocks allogeneic mononuclear cell activation and cytokine production in vivo and prolongs rat cardiac allograft survival. Hancock, W.W., Whitley, D., Kupiec-Weglinski, J.W., Tilney, N.L. Transplant. Proc. (1992) [Pubmed]
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