RESEARCH INTERESTS

Total synthesis

Enzyme model studies

Cancer chemotherapy

Role of metals in diseases

Synthetic methods, polyamines

Metal chelators

Membrane transport

AREAS OF TECHNICAL EXPERTISE

Organic synthesis

High-field NMR

Cell culture

Animal models

Iron chelation

Polyamine biochemistry

Organic synthesis

1. Badman D.G., Bergeron R.J., Brittenham G.M.  Iron Chelators: New Development Strategies. Eds.  Saratoga Publishing, Inc., Saratoga, WY (2000).
2. Bergeron R.J., Brittenham G.M.  The Development of Iron Chelators for Clinical Use.  Eds. CRC Press, Inc.: Boca Raton, FL  (1994).
3. Bender M.L., Bergeron R.J., Komiyama M.  The Bioorganic Chemistry of Enzymatic Catalysis.  John Wiley and Sons: New York, NY (1984).

1. Bergeron R.J. Huang G., Weimar W.R., Smith R.E., Wiegand J., McManis J.S. “Desferrithiocin Analogue-based Hexacoordinate Iron(III) Chelators.”  J. Med. Chem., in press.
2. Bergeron R.J. Wiegand J., Weimar W.R., Nguyen J.N., Sninsky C.A.  “Prevention of Acetic Acid-induced Colitis by Desferrithiocin Analogs in a Rat Model.”  Dig. Dis. Sci., in press.
3. Bergeron R.J. McManis J.S., Weimar W.R., Wiegand J., Eiler-McManis E.  “Iron Chelators and Therapeutic Uses.”  Burger’s Medicinal Chemistry, 6th ed., Wiley, New York, in press.
4. Bergeron R.J.  “Hydroxylation of Desazadesferrithiocin Analogues: A Structure–Activity Study.” Hematology 2001, American Society of Hematology, Washington, D. C., (Online at www.hematology.org), in press.
5. Roberts S.M., Weimar W.R., Vinson J.R.T., Munson J.W., Bergeron J.R.  “Measurement of Arsenic Bioavailability in Soil Using a Primate Model.”  Toxicol. Sci., 67:303–310 (2002).
6. Bergeron R.J. Wiegand J., Brittenham G.M.  “HBED:  Preclinical Studies of a Potential Alternative to Deferoxamine for Treatment of Chronic Iron Overload and Acute Iron Poisoning.”  Blood, 99(8):3019-3026 (2002).
7. Bergeron R.J. Wiegand J., McManis J.S., Weimar W.R., Huang G.  “Structure–Activity Relationships Among Desazadesferrithiocin Analogues.” Iron Chelation Therapy, Kluwer Academic/Plenum, New York, (2002).
8. Bergeron R.J., Wiegand J., Fannin T.L.  “Control of Irritable Bowel Syndrome with Polyamine Analogues: A Structure–Activity Study.” Dig. Dis. Sci., 46(12):2615–2623 (2001).
9. Bergeron R.J., Xin M.G., Weimar W.R., Smith R.E., Wiegand J.  “Significance of Asymmetric Sites in Choosing Siderophores as Deferration Agents.”  J. Med. Chem., 44(15):2469-2478 (2001).
10. Bergeron R.J., Müller R., McManis J.S., Yao G.W., Huang G.  “An Improved Synthesis of (3S,12S)-N1,N14-Diethyl-3,12-dihydroxyhomospermine, a Polyamine Analogue Therapeutic Agent.” Synthesis, (7):1043–1048 (2001).
11. Bergeron R.J., Müller R., Huang G., McManis J.S., Algee S.E., Yao H., Weimar W.R., Wiegand J.  “Synthesis and Evaluation of Hydroxylated Polyamine Analogues as Antiproliferatives.” J. Med. Chem., 44(15):2451–2459 (2001).
12. Bergeron R.J., Wiegand J., McManis J.S., Weimar W.R., Smith R.E., Algee S.E., Fannin T.L., Slusher M.A., Snyder P.S.  “Polyamine Analogue Antidiarrheals: A Structure–Activity Study.”  J. Med. Chem., 44(2):232–244 (2001).
13. Rao L., Choppin G.R., Bergeron R.J.  “Complexation of Thorium(IV) with Desmethyldesferrithiocin.”  Radiochim. Acta, 88:851–856 (2000).
14. Bergeron R.J., Merriman R.L., Olson S.G., Wiegand J., Bender J., Streiff R.R., Weimar W.R.  “Metabolism and Pharmacokinetics  of N1,N11-Diethylnorspermine in a Cebus apella Primate Model.”  Cancer Res., 60(16):4433–4439 (2000).
15. Bergeron R.J., Müller R., Bussenius J., McManis J.S., Merriman R.L., Smith R.E., Yao H., Weimar W.R.  “Synthesis and Evaluation of Hydroxylated Polyamine Analogues as Antiproliferatives.”  J. Med. Chem., 43(2):224–235 (2000).
16. Bergeron R.J., McManis J.S., Wiegand J., Weimar W.R.  “A Search for Clinically Effective Iron Chelators.”  Iron Chelators: New Development Strategies, Saratoga Publishing, Inc., Saratoga, pp. 253–292 (2000).
17. Bergeron R.J., Weimar W.R., Wiegand J.  “Pharmacokinetics of Orally Administered Desferrithiocin Analogs in Cebus apella Primates.”  Drug Metab. Dispos., 27(12):1496–1498 (1999).
18. Brittenham G.M., Bergeron R.J., Fujioka H., Looareesuwan S., Wilairatana P., Pootrakul P., Asawamahasakda W., Yuthavong Y., Meshnick S., Gordeuk V.R., Aikawa M.  “Antimalarial Iron-Chelating Agents Based on Desferrithiocin.”  Measuring the Impact of Tropical Diseases and Outcomes, U.S. Department of Health and Human  Services, National Institutes of Health, Bethesda, Maryland (1999).
19. Bergeron R.J., Bussenius J., Müller R., McCosar B.H., McManis J.S., “(R)- and (S)-N-(Benzyloxycarbonyl)-3,4-epoxybutylamine. New 4-Amino-2-hydroxybutyl Synthons for the Synthesis of Hypusine Reagents and (R)-6- and (S)-7-Hydroxyspermidine.”  Tetrahedron: Asymmetry, 10(22):4285–4294 (1999).
20. Bergeron R.J., Wiegand J., McManis J.S., McCosar B.H., Weimar W.R., Brittenham G.M., Smith R.E.  “Effects of C-4 Stereochemistry and C-4' Hydroxylation on the Iron Clearing Efficiency and Toxicity of Desferrithiocin Analogues.” J. Med. Chem., 42:2432–2440 (1999).
21. Bergeron R.J., McManis J.S., Bussenius J., Brittenham G.M., Wiegand J.  “Evaluation of the Desferrithiocin Pharmacophore as a Vector for Hydroxamates.”  J. Med. Chem., 42(15):2881–2886 (1999).
22. Kramer D.L., Vujcic S., Diegelman P., Alderfer J., Miller J.T., Black J.D., Bergeron R.J., Porter C.W.  “Polyamine Analogue Induction of the p53-p21WAF1CIP1-Rb Pathway and G1 Arrest in Human Melanoma Cells.”  Cancer Res., 59:1278–1286 (1999).
23. Bergeron R.J., Wiegand J., Brittenham G.M.  “HBED:  The Continuing Development of A Potential Alternative to Deferoxamine for Iron-Chelating Therapy.”  Blood, 93(1):370–375 (1999).
24. Bergeron R.J., Wiegand J., Weimar W.R., Vinson J.R.T., Bussenius J., Yao G.W., McManis J.S.  “Desazadesmethyldesferrithiocin Analogues as Orally Effective Iron Chelators.”  J. Med. Chem., 42:95–108 (1999).
25. Bergeron R.J., Weimar W.R., Müller R., Zimmerman C.O., McCosar B.H., Yao H., Smith R.E. “Effect of Polyamine Analogues on Hypusine Content in JURKAT T-Cells.”  J. Med. Chem., 41(20):3901-3908 (1998).
26. Bergeron R.J., Weimar W.R., Müller R., Zimmerman C.O., McCosar B.H., Yao H., Smith R.E.  “Synthesis of Reagents for the Construction of Hypusine and Deoxyhypusine Peptides and their Application as Peptidic Antigens.”  J. Med. Chem., 41(20):3888-3900 (1998).
27. Kramer D.L., Black J.D., Mett H., Bergeron R.J., Porter C.W.  “Lysosomal Sequestration of Polyamine Analogs in Chinese Hamster Ovary Cells Resistant to the S-Adenosylmethionine Decarboxylase Inhibitor CGP-48664.”  Cancer Res., 58:3883–3890 (1998).
28. Bergeron R.J., Wiegand J., Brittenham G.M., “HBED:  A Potential Alternative to Deferoxamine for Iron-Chelating Therapy.”  Blood, 91(4):1446-1452 (1998).
29. Bergeron R.J., Wiegand J., Weimar W.R., Snyder P.S.  “Polyamine Analogue Antiarrhythmics.” Pharm. Res., 38(5):367-380 (1998).