Raymond Bergeron Ph.D.
Duckworth Professor of Drug Development
Graduate Research Professor, Ph.D.
Brandeis University, Waltham, MA, 1972
Research Interests
- total synthesis
- enzyme model studies
- cancer chemotherapy
- role of metals in diseases
- synthetic methods, polyamines
- metal chelators
- membrane transport
Ongoing research is in the areas of cancer chemotherapy, the
role of metals in diseases and metal chelators.
Other special capabilities are: high field NMR, cell culture and
enzymology.
Sample Publications
1. "Protection and Monoalkylation of Amines." J. B. Hendrickson and R. J. Bergeron, Tetrahedron Lett., 5, 345-348 (1970).
2. "Triflamides (CF3SO2N). A Survey." J. B. Hendrickson, R. J. Bergeron, A. Giga, and D. Sternbach, J. Amer. Chem. Soc., 95, 3412-3413 (1973).
3. "A New Thermal Pericyclic Carbon Transfer Capable of Creating Quaternary Sites." J. B. Hendrickson and R. J. Bergeron, Tetrahedron Lett., 37, 3609-3610 (1973).
4. "Triflamides for Protection and Monoalkylation of Amines and a New Gabriel Synthesis." J. B. Hendrickson and R. J. Bergeron, Tetrehedron Lett., 39, 3839-3842 (1973).
5. "Triflamides: New Acylating and Triflating Reagents." J. B. Hendrickson and R. J. Bergeron, Tetrahedron Lett., 46, 4607-4610 (1973).
6. "Effects of Cyclodextrins on Fatty Acid Synthesis." Y. Machida, R. J. Bergeron, P. Flick, and K. Bloch, J. Biol. Chem., 248, 6246-6247 (1973).
7. "New 'Gabriel' Syntheses of Amines." J. B. Hendrickson, R. J. Bergeron, and D. D. Sternbach, Tetrahedron, 31, 2517-2521 (1975).
8. "Complex Formation Between Mycobacterial Polysaccharides or Cyclodextrins and Palmitoyl Coenzyme A." R. J. Bergeron, Y. Machida, and K. Bloch, J. Biol. Chem., 250, 1223-1230 (1975).
9. "Selective Alkylation of Cycloheptaamylose." R. J. Bergeron, M. Meeley, and Y. Machida, Bioorg. Chem., 5, 121-126 (1976).
10. "The Role of Strain Energy in Cycloamylose Substrate Complexation." R. J. Bergeron and M. Meeley, Bioorg. Chem., 5, 197-202 (1976).
11. "The Molecular Disposition of Sodium p-Nitrophenolate in the Cavities of Cycloheptaamylose and Cyclohexaamylose in Solution." R. J. Bergeron and R. Rowan, III, Bioorg. Chem., 5, 425-436 (1976).
12. "The Molecular Disposition of p-Nitrophenol and Sodium p-Nitrophenolate in the Cyclohexaamylose Cavity: A 13C Probe." R. J. Bergeron and M. A. Channing, Bioorg. Chem., 5, 437-439 (1976).
13. "Cycloamyloses." R. J. Bergeron, J. Chem. Ed., 54, 204-207 (1977).
14. "Disposition Requirements for Binding in Aqueous Solution of Polar Substrates in the Cyclohexaamylose Cavity." R. J. Bergeron, M. A. Channing, G. J. Gibeily, and D. M. Pillor, J. Amer. Chem. Soc., 99, 5146-5151 (1977).
15. "Circular Dichroism Studies on the Structure of p-Nitrophenolate Cycloamylose Complexes." R. J. Bergeron and P. McPhie, Bioorg. Chem., 6, 465-471 (1977).
16. "Uses of the Trifyl [trifluoromethanesulfonyl] Group in Organic Synthesis. A Review." J. B. Hendrickson, K. W. Bair, R. J. Bergeron, A. Giga, P. L. Skipper, D. D. Sternbach, and J. A. Wareing, Org. Prep. Proc. Int., 9, 173-207 (1977).
17. "Thermodynamics of Cycloamylose-Substrate Complexation." R. J. Bergeron, D. M. Pillor, G. Gibeily, and W. P. Roberts, Bioorg. Chem., 7, 263-271 (1978).
18. "Dependence of Cycloamylose-Substrate Binding on Charge." R. J. Bergeron, M. A. Channing, and K. A. McGovern, J. Amer. Chem. Soc., 100, 2878-2883 (1978).
19. "Boundary Conditions for the Hildebrand-Benesi Equation." R. J. Bergeron and W. P. Roberts, Anal. Biochem., 90, 844-848 (1978).
20. "Mild Oxidation of Alkyl Halides." R. J. Bergeron and P. G. Hoffman, J. Org. Chem., 44, 1835-1839 (1979).
21. "Carboxylate Anion Binding in the Cyclohexaamylose Cavity: A Steric and Electronic Evaluation." R. J. Bergeron, M. A. Channing, K. A. McGovern, and W. P. Roberts, Bioorg. Chem., 8, 263-281(1979).
22. "Importance of Cycloamylose Substrate Geometry and Dynamic Coupling in the Deacylation of 3- and 4-Nitrophenyl Acetates." R. J. Bergeron and M. A. Channing, J. Amer. Chem. Soc., 101, 2511-2516 (1979).
23. "Application of N-Phenyltrifluoromethanesulfonamides to the Synthesis of Pyrazines." R. J. Bergeron and P. G. Hoffman, J. Org. Chem., 45, 161-163 (1980).
24. "Application of N-Phenyltriflamide to the Synthesis of Deoxyaspergillic Acid." R. J. Bergeron and P. G. Hoffman, J. Org. Chem., 45, 163-165 (1980).
25. "Synthesis of N4-Acylated N1,N8-Bis(acyl)Spermidines: An Approach to the Synthesis of Siderophores." R. J. Bergeron, K. A. McGovern, M. A. Channing, and P. S. Burton, J. Org. Chem., 45,1589-1592 (1980).
26. "Synthesis, Absorption and Toxicity of N1,N8-Bis(2,3-dihydroxybenzoyl)Spermidine, a Potent Iron Chelator." R. J. Bergeron, P. S. Burton, K. A. McGovern, E. J. St. Onge, and R. R. Streiff, J. Med. Chem., 23, 1130-1133 (1980).
27. "Biomimetic Synthesis of a Paracoccus Denitrificans Siderophore Analogue." R. J. Bergeron, P. S. Burton, S. J. Kline, and K. A. McGovern, J. Org. Chem., 46, 3712-3718 (1981).
28. "Reagents for the Selective Acylation of Spermidine, Homospermidine and Bis-[3-amino- propylamine." R. J. Bergeron, P. S. Burton, K. A. McGovern, and S. J. Kline, Synthesis, 732-733 (1981).
29. "Flexible Synthesis of Polyamine Catecholamides." R. J. Bergeron, S. J. Kline, N. J. Stolowich, K. A. McGovern, and P. S. Burton, J. Org. Chem., 46, 4524-4529 (1981).
30. "Role of Cyclohexaamylose C-3 Hydroxyls in Catalytic Hydrolysis." R. J. Bergeron and P. S. Burton, J. Amer. Chem. Soc., 104, 3664-3670 (1982).
31. "Fluorescent Lipoprotein Probe." R. J. Bergeron and J. Scott, Anal. Biochem., 119, 128-134 (1982).
32. "Cholestatriene and Ergostatetraene as in vivo and in vitro Membrane and Lipoprotein Probes." R. J. Bergeron and J. Scott, J. Lipid Res., 23, 391-404 (1982).
33. "Short Synthesis of Parabactin." R. J. Bergeron and S. J. Kline, J. Amer. Chem. Soc., 104, 4489-4492 (1982).
34. "Biological Properties of N4-Spermidine Derivatives and their Potential in Anticancer Chemotherapy." C. W. Porter, R. J. Bergeron, and N. J. Stolowich, Cancer Res., 42, 4072- 4078 (1982).
35. "Reagents for the Selective Secondary N-Acylation of Linear Triamines." R. J. Bergeron, N. J. Stolowich, and C. W. Porter, Synthesis, 689-692 (1982).
36. "Spermidine Requirement for Cell Proliferation in Eukaryotic Cells: Structural Specificity and Quantitation." C. W. Porter and R. J. Bergeron, Science, 219, 1083-1085 (1983).
37. "Synthesis and Solution Dynamics of Agrobactin A." R. J. Bergeron, N. J. Stolowich, and S. J. Kline, J. Org. Chem., 48, 3432-3439 (1983).
38. "Bacteriostatic and Fungiostatic Action of Catecholamide Iron Chelators." R. J. Bergeron, G. S. Elliott, S. J. Kline, R. Ramphal, and L. St. James, III, Antimicrob. Agents Chemother., 24, 725-730 (1983).
39. "Catecholamide 'H-shaped' Ligands as Actinide Chelators." R. J. Bergeron, S. J. Kline, J. Navratil, and C.M. Smith, Radiochim. Acta, 35, 47-51 (1984).
40. "300 MHz 1H NMR Study of Parabactin and its Gallium(III) Chelate." R. J. Bergeron and S. J. Kline, J. Amer. Chem. Soc., 106, 3089-3098 (1984).
41. "Amines and Polyamines from Nitriles." R. J. Bergeron and J. R. Garlich, Synthesis, 782- 784 (1984).
42. "Reagents for the Stepwise Functionalization of Spermidine, Homospermidine and Bis-(3- aminopropyl)amine." R. J. Bergeron, J. R. Garlich, and N. J. Stolowich, J. Org. Chem., 49, 2997-3001 (1984).
43. "Treatment With alpha-Difluoromethylornithine Plus a Spermidine Analogue Leads to Spermine Depletion and Growth Inhibition in Cultured L1210 Leukemia Cells." R. Casero, R. J. Bergeron, and C. W. Porter, J. Cell. Physiol., 121, 476-482 (1984).
44. "Cycloamylose-Substrate Binding." R. J. Bergeron, Inclusion Compounds III, Chapter 12, J. L. Atwood, J. E. D. Davies and D. D. MacNicol, eds. Academic: London, UK (1984).
45. "Aliphatic Chain Length Specificity of the Polyamine Transport System in Ascites L1210 Leukemia Cells." C. W. Porter, J. Miller, and R. J. Bergeron, Cancer Res., 44, 126-128 (1984).
46. "Antineoplastic and Antiherpetic Activity of Spermidine Catecholamide Iron Chelators." R. J. Bergeron, P. F. Cavanaugh, Jr., S. J. Kline, R. G. Hughes, Jr., G. T. Elliott, and C. W. Porter, Biochem. Biophys. Res. Comm., 121, 848-854 (1984).
47. "Synthesis and Solution Structures of Microbial Siderophores." R. J. Bergeron, Chem. Rev., 84, 587-602 (1984).
48. "Biological Properties of N4- and N1, N8-Spermidine Derivatives in Cultured L1210 Leukemia Cells." C. W. Porter, P. F. Cavanaugh, N. J. Stolowich, B. Ganis, E. Kelly, and R. J. Bergeron, Cancer Res., 45, 2050-2057 (1985).
49. "An Efficient Total Synthesis of Agrobactin and its Gallium(III) Chelate." R. J. Bergeron, J. S. McManis, J. B. Dionis, and J. R. Garlich, J. Org. Chem., 50, 2780-2782 (1985).
50. "Total Synthesis of Vibriobactin." R. J. Bergeron, J. R. Garlich, and J. S. McManis, Tetrahedron, 41, 507-510 (1985).
51. "Mechanism and Stereospecificity of the Parabactin-Mediated Iron-Transport System in Paracoccus Denitrificans." R. J. Bergeron, J. B. Dionis, G. T. Elliot, and S. J. Kline, J. Biol. Chem., 260, 13, 7936-7944 (1985).
52. "Influence of Iron on in vivo Proliferation and Lethality of L1210 Cells." R. J. Bergeron, R. R. Streiff, and G. T. Elliott, J. Nutr., 115, 369-374 (1985).
53. "Characterization of L1210 Cell Growth Inhibition by the Bacterial Iron Chelators Parabactin and Compound II." P. F. Cavanaugh, Jr., C. W. Porter, D. Tukalo, O. S. Frankfurt, Z. P. Pavelic, and R. J. Bergeron, Cancer Res., 45, 4754-4759 (1985).
54. "Methods for the Selective Modification of Spermidine and its Homologues." R. J. Bergeron, Accts. Chem. Res., 19, 105-113 (1986).
55. "Iron: A Controlling Nutrient in Proliferative Processes." R. J. Bergeron, Trends in Biochem. Sci., 11, 133-136 (1986).
56. "Effects of the Vibrio Cholerae Siderophore Vibriobactin on the Growth Characteristics of L1210 Cells." R. J. Bergeron, R. Braylan, S. Goldey, and M. J. Ingeno, Biochem. Biophys. Res. Comm., 136, 273-280 (1986).
57. "Hexahydropyrimidines as Masked Spermidine Vectors in Drug Delivery." R. J. Bergeron and H. W. Seligsohn, Bioorg. Chem., 14, 345-355 (1986).
58. "Comparison and Characterization of Growth Inhibition in L1210 Cells by alpha-Difluoromethylornithine (DFMO), an Inhibitor of Ornithine Decarboxylase, and N1,N8-Bis(ethyl)Spermidine, an Apparent Regulator of the Enzyme." C. W. Porter, B. Ganis, T. Vinson, L. J. Marton, D. L. Kramer, and R. J. Bergeron, Cancer Res., 46, 6279- 6285 (1986).
59. "Catecholamide Chelators for Actinide Environmental and Human Decontamination." R. J. Bergeron and J. D. Navratil. Chemical Separations, Volume II, Applications: C. J. King and J. T. Navratil (Eds.), Litarvan Literature: Denver, CO (1986).
60. "Synthesis of a Parabactin Photoaffinity Label." R. J. Bergeron, J. B. Dionis, and M. J. Ingeno, J. Org. Chem., 52, 144-149 (1987).
61. "Synthesis and Properties of Polyamine Catecholamide Chelators." R. J. Bergeron, Iron Transport in Microbes, Plants and Animals, Chapter 16, G. Winklemann, D. Vander Helm, J. B. Neilands (Eds.), VCH Verlagsgsellschaft/VCH Publishers, 285-315 (1987).
62. "Structural Determinants of Spermidine-DNA Interactions." P. M. Vertino, R. J. Bergeron, P. F. Cavanaugh, Jr., and C. W. Porter, Biopolymers, 26, 691-703 (1987).
63. "Relative Abilities of Bis(ethyl) Derivatives of Putrescine, Spermidine, and Spermine to Regulate Polyamine Biosynthesis and Inhibit L1210 Leukemia Cell Growth." C. W. Porter, J. McManis, R. A. Casero, and R. J. Bergeron, Cancer Res., 47, 2821-2825 (1987).
64. "Total Synthesis of (±)-15-Deoxyspergualin." R. J. Bergeron and J. S. McManis, J. Org. Chem., 52, 1700-1703 (1987).
65. "Microbial Iron Chelator-Induced Cell Cycle Synchronization in L1210 Cells: Potential in Combination Chemotherapy." R. J. Bergeron and M. J. Ingeno, Cancer Res., 47, 6010-6016 (1987).
66. "Regulation of Ornithine Decarboxylase Activity by Spermidine and the Spermidine Analogue N1N8-Bis(ethyl)Spermidine." C. W. Porter, F. G. Berger, A. E. Pegg, B. Ganis, and R. J. Bergeron, Biochem. J., 242, 433-440 (1987).
67. "Synthetic Polyamine Analogues as Antineoplastics." R. J. Bergeron, A. H. Neims, J. S. McManis, T. R. Hawthorne, J. R. T. Vinson, R. Bortell, and M. J. Ingeno, J. Med. Chem., 31, 1183-1190 (1988).
68. "Demonstration of Ferric L-Parabactin Binding Activity in the Outer Membrane of Paracoccus Denitrificans." R. J. Bergeron, W. R. Weimar, and J. B. Dionis, J. Bacteriol., 170, 3711-3717 (1988).
69. "Control of Ornithine Decarboxylase Activity in alpha-Difluoromethylornithine-Resistant L1210 Cells by Polyamines and Synthetic Analogues." A. E. Pegg, R. Madhubala, T. Kameji, and R. J. Bergeron, J. Biol. Chem., 263, 11008-11014 (1988).
70. "Reagents for the Stepwise Functionalization of Spermine." R. J. Bergeron and J. S. McManis, J. Org. Chem., 53, 3108-3111 (1988).
71. "Selective Regulation of S-Adenosylmethionine Decarboxylase Activity by the Spermine Analogue 6-Spermyne." C. W. Porter, J. S. McManis, D. Lee, and R. J. Bergeron, Biochem. J., 254, 337-342 (1988).
72. "Enzyme Regulation as an Approach to Interference with Polyamine Biosynthesis-An Alternative to Enzyme Inhibition." C. W. Porter and R. J. Bergeron, Adv. Enz. Regul., 27, 57-79 (1988).
73. "Regulation of Polyamine Biosynthetic Activity by Spermidine and Spermine Analogues- A Novel Antiproliferative Strategy." C. W. Porter and R. J. Bergeron, Adv. Exp. Med. Biol., 250, (Progress in Polyamine Research), V. Zappia and A. E. Pegg, Eds., Plenum Publishing Corp. 677-690 (1988).
74. "Modulation of Polyamine Biosynthesis and Transport by Oncogene Transfection." B. K. Chang, P. R. Libby, R. J. Bergeron, and C. W. Porter, Biochem. Biophys. Res. Comm., 157, 264-270 (1988).
75. "An Efficient Total Synthesis of Desferrioxamine B." R. J. Bergeron and J. J. Pegram, J. Org. Chem., 53, 3131-3134 (1988).
76. "Combination Iron Depletion Therapy." R. Taetle, J. M. Honeysett, and R. J. Bergeron, J. Nat. Cancer Inst., 81, 1229-1235 (1989).
77. "Differential Response to Treatment with the Bis(ethyl)Polyamine Analogues Between Human Small Cell Lung Carcinoma and Undifferentiated Large Cell Lung Carcinoma in Culture." R. A. Casero, Jr., S. J. Ervin, P. Celano, S. B. Baylin, and R. J. Bergeron, Cancer Res., 49, 639-643 (1989).
78. "Role of the Methylene Backbone in the Antiproliferative Activity of Polyamine Analogues on L1210 Cells." R. J. Bergeron, T. R. Hawthorne, J. R. T. Vinson, D. E. Beck, Jr., and M. J. Ingeno, Cancer Res., 49, 2959-2964 (1989).
79. "Effect of N1, N12-Bis(ethyl)Spermine and Related Compounds on Growth and Polyamine Acetylation, Content and Excretion in Human Colon Tumor Cell." A. E. Pegg, R. Wechter, R. Pakala, and R. J. Bergeron, J. Biol. Chem., 264, 11744-11749 (1989).
80. "Differential Induction of Spermidine/Spermine N1-Acetyltransferase in Human Lung Cancer Cells by the Bis(ethyl)Polyamine Analogues." R. A. Casero, Jr., P. Celano, S. J. Ervin, C. W. Porter, R. J. Bergeron, and P. Libby, Proc. Am. Assoc. Cancer Res., 49, 3829- 3833 (1989).
81. "The Total Synthesis of Bisucaberin." R. J. Bergeron and J. S. McManis, Tetrahedron, 45, 4939-4944 (1989).
82. "Major Increases in Spermidine/Spermine-N1-Acetyltransferase Activity by Spermine Analogues and their Relationship to Polyamine Depletion and Growth Inhibition in L1210 Cells." P. R. Libby, M. Henderson, R. J. Bergeron, and C. W. Porter, Cancer Res., 49, 6226-6231 (1989).
83. "Correlation Between the Effects of Polyamine Analogues on DNA Conformation and Cell Growth." H. S. Basu, B. G. Feuerstein, D. F. Deen, W. P. Lubich, R. J. Bergeron, K. Samejima, and L. J. Marton, Cancer Res., 49, 5591-5597 (1989).
84. "Structure-Function Correlations of Polyamine Analog-Induced Increases in Spermidine/Spermine Acetyltransferase Activity." P. R. Libby, R. J. Bergeron, and C. W. Porter, Biochem. Pharmacol., 38, 1435-1442 (1989).
85. "Effect of N1, N14-Bis-(ethyl)-Homospermine on the Growth of U-87 MG and SF-126 Human Brain Tumor Cells." H. S. Basu, M. Pellarin, B. G. Feuerstein, D. F. Deen, R. J. Bergeron, and L. J. Marton, Cancer Res., 50, 3137-3140 (1990).
86. "Kinetics of Iron Acquisition from Ferric Siderophores by Paracoccus Denitrificans." R. J. Bergeron and W. R. Weimar, J. Bacteriol., 172, 2650-2657 (1990).
87. "A Comparative Evaluation of Iron Clearance Models." R. J. Bergeron, R. R. Streiff, J. Wiegand, J. R. T. Vinson, G. Luchetta, K. M. Evans, H. H. Peter, and H.-B. Jenny, Ann. N. Y. Acad. Sci., 612, 378-393 (1990).
88. "Combined Regulation of Ornithine and S-Adenosylmethionine Decarboxylases by Spermine and the Spermine Analogue N1,N12-Bis(ethyl)Spermine." C. W. Porter, A. E. Pegg, B. Ganis, R. Madhabala, and R. J. Bergeron, Biochem. J., 268, 207-212 (1990).
89. "Induction of Spermidine/Spermine N1-Acetyltransferase Activity in Chinese- Hamster Ovary cells by N1,N11-Bis(ethyl)Norspermine and Related Compounds." A. E. Pegg, R. Pakala, and R. J. Bergeron, Biochem. J., 267(3), 331-338 (1990).
90. "The Total Synthesis of Desferrioxamines E and G." R. J. Bergeron and J. S. McManis, Tetrahedron, 46, 5881-5888 (1990).
91. "Increase in Spermine Content Coordinated With Siderophore Production in Paracoccus Denitrificans." R. J. Bergeron and W. R. Weimar, J. Bacteriol., 173, 2238-2243 (1991).
92. "Selective Cellular Depletion of Mitochondrial DNA by the Polyamine Analog, N1,N12- Bis(ethyl)Spermine, and its Relationship to Polyamine Structure and Function." P. M. Vertino, T. A. Beerman, E. J. Kelly, R. J. Bergeron, and C. W. Porter, Mol. Pharm., 39, 487-494 (1991).
93. "Characterization of Human Spermidine/Spermine N1-Acetyltransferase Purified from Cultured Melanoma Cells." P. R. Libby, B. Ganis, R. J. Bergeron, and C. W. Porter, Arch. Biochem. Biophys., 284, 238-244 (1991).
94. "Synthesis of Catecholamide and Hydroxamate Siderophores." R. J. Bergeron and J. S. McManis, CRC Handbook on Microbial Iron Chelates 1991, pp. 271-307 (1991).
95. "Evaluation of Desferrithiocin and its Synthetic Analogues as Orally Effective Iron Chelators." R. J. Bergeron, J. Wiegand, J. B. Dionis, M. Egli-Karmakka, J. Frei, A. Huxley-Tencer, and H. H. Peter, J. Med. Chem., 34, 2072-2078 (1991).
96. "The Total Synthesis of Alcaligin." R. J. Bergeron, J. S. McManis, P.T. Perumal, and S. E. Algee, J. Org. Chem, 56, 5560-5563 (1991).
97. "The Synthesis and Biological Evaluation of Hydroxamate-Based Iron Chelators." R. J. Bergeron, J. Wiegand, J. S. McManis, and P. T. Perumal, J. Med Chem., 34, 3182-3187 (1991).
98. "Cellular Responses to Polyamine Analogues and Inhibitors in Human Pancreatic Adenocarcinoma Cell Lines." B. K. Chang, C. W. Porter, and R. J. Bergeron, J. Cellular Pharmacol. 2, 133-137 (1991).
99. "Correlations Between Polyamine Analog-Induced Increases in Spermidine/Spermine N1- Acetyltransferase Activity, Polyamine Pool Depletion, and Growth Inhibition in Human Melanoma Cell Lines." C. W. Porter, B. Ganis, P. R. Libby, and R. J. Bergeron, Cancer Res., 51, 3715-3720 (1991).
100. "A Comparison of the Iron-Clearing Properties of 1, 2-Dimethyl-3-hydroxypyrid-4-one, 1, 2-Diethyl-3-hydroxypyrid-4-one, and Deferoxamine." R. J. Bergeron, R. R. Streiff, J. Wiegand, G. Luchetta, E. A. Creary, and H. H. Peter, Blood, 79, 1882-1890 (1992).
101. "Regulation of Polyamine Biosynthetic Activity and Homeostasis as a Novel Antiproliferative Strategy." C. W. Porter, D. L. Kramer, R. J. Bernacki, and R. J. Bergeron, Dev. Oncol., 68, 325-344 (1992).
102. "Differential Effects of the Spermine Analog, N1,N12 Bis(ethyl) Spermine, on Polyamine Metabolism and Cell Growth in Human Melanoma Cell Lines and Melanocytes." N. W. Shappell, J. T. Miller, R. J. Bergeron and C. W. Porter, Anticancer Res., 12, 1083-1090 (1992).
103. "Antitumor Effects of N-Alkylated Polyamine Analogs in Human Pancreatic Adenocarcinoma Models." B. K. Chang, R. J. Bergeron, C. W. Porter, and Y. Liang, Cancer Chemother. Pharmacol., 30, 179-182 (1992).
104. "Regulatory and Antiproliferative Effects of N-Alkylated Polyamine Analogs in Human and Hamster Pancreatic Adenocarcinoma Cell Lines." B. K. Chang, R. J. Bergeron, C. W. Porter, J. R. T. Vinson, Y. Liang, and P. R. Libby, Cancer Chemother. Pharmacol., 30, 183-188 (1992).
105. "Antitumor Activity of N, N'-Bis(ethyl)Spermine Homologues Against Human MALME-3 Melanoma Xenografts." R. J. Bernacki, R. J. Bergeron, and C. W. Porter, Cancer Res., 52, 2424-2430 (1992).
106. "Polyamine Analogues in Pancreatic Adenocarcinoma: A Strategy for Effective Antitumor Therapy in Chemoresistant Gastrointestinal Malignancies." B. K. Chang, R. J. Bergeron, C. W. Porter, and J. R. T. Vinson, Falk Symposium on Polyamines in the Gastrointestinal Tract, 62, 173-186 Kluwer Press, Lancaster, U.K. (1992).
107. "Polyamine Inhibitors and Analogues as Potential Anticancer Agents." C. W. Porter, U. Regenass, and R. J. Bergeron, Falk Symposium on Polyamines in the Gastrointestinal Tract, 62, 301-322 Kluwer Press, Lancaster, U.K. (1992).
108. "The Total Synthesis of Nannochelin: A Novel Cinnamoyl Hydroxamate-Containing Siderophore." R. J. Bergeron and O. Phanstiel, IV, J. Org. Chem., 57, 7140-7143 (1992).
109. "Structural Alterations in Desferrioxamine Compatible with Iron Clearance in Animals." R. J. Bergeron, Z. R. Liu, J. S. McManis, and J. Wiegand, J. Med. Chem., 35, 4739-4744 (1992).
110. "Steady-State Messenger RNA and Activity Correlates With Sensitivity to N1,N12- Bis(ethyl)Spermine in Human Cell Lines Representing the Major Forms of Lung Cancer." R. A. Casero, Jr., A. R. Mank, L. Xiao, J. Smith, R. J. Bergeron, and P. Celano, Cancer Res., 52, 5359-5363 (1992).
111. "Regulation of Polyamine Transport by Polyamines and Polyamine Analogs." D. L. Kramer, J. T. Miller, R. J. Bergeron, R. Khomutov, A. Khomutov, and C. W. Porter, J. Cell. Physiol., 155, 399-407 (1993).
112. "Effects of Diethylspermine Analogues in Human Bladder Cancer Cell Lines in Culture." B. K. Chang, Y. Liang, D. W. Miller, R. J. Bergeron, C. W. Porter, and G. Wang, J. Urol., 150, 1293-1297 (1993).
113. "Growth Inhibition of Hormone-Responsive and -Resistant Human Breast Cancer Cells in Culture by N1,N12-Bis(ethyl)Spermine." N. E. Davidson, A. R. Mank, L. J. Prestigiacomo, R. J. Bergeron, and R. A. Casero, Jr., Cancer Res., 53, 2071-2075 (1993).
114. "A Comparative Study of the Iron-Clearing Properties of Desferrithiocin Analogs With Desferrioxamine B in a Cebus Monkey Model." R. J. Bergeron, R. R. Streiff, E. A. Creary, R. D. Daniels, Jr., W. King, G. Luchetta, J. Wiegand, T. Moerker, and H. H. Peter, Blood, 81, 2166-2173 (1993).
115. "Antitumor Activity of N1,N11-Bis(ethyl)Norspermine Against Human Melanoma Xenografts and Possible Biochemical Correlates of Drug Action." C. W. Porter, R. J. Bernacki, J. Miller, and R. J. Bergeron, Cancer Res., 53, 581-586 (1993).
116. "Investigations of the Mechanism by which Mammalian Cell Growth is Inhibited by N1,N12- Bis(ethyl)Spermine." L. Albanese, R. J. Bergeron, and A. E. Pegg, Biochem. J., 291, 131- 137 (1993).
117. "Toward Better Chelation Therapy: Current Concepts and Research Strategy." H.-P. Schnebli, I. Hassan, K. O. Hamilton, S. Lynch, Y. Jin, H. P. Nick, H. H. Peter, U. Junker Walker, R. Ziel, S. C. Khanna, R. Dean, and R. J. Bergeron, The Development of Iron Chelators for Clinical Use, CRC Press, Inc., Boca Raton, pp. 131-149 (1994).
118. "Synthesis and Biological Activity of Hydroxamate-Based Iron Chelators." R. J. Bergeron and J. S. McManis, The Development of Iron Chelators for Clinical Use, CRC Press, Inc., Boca Raton, pp. 237-273 (1994).
119. "A Comparative Evaluation of Iron Chelators in a Primate Model." H. H. Peter, R. J. Bergeron, R. R. Streiff, and J. Wiegand, The Development of Iron Chelators for Clinical Use, CRC Press, Inc., Boca Raton, pp. 373-394 (1994).
120. "A Comparison of the Iron-Clearing Properties of Parabactin and Desferrioxamine." R. J. Bergeron, R. R. Streiff, W. King, R. D. Daniels, Jr, and J. Wiegand, Blood, 82, 2552- 2557 (1993).
121. "Radiopotentiation of Human Brain Tumor Cells by the Spermine Analog N1,N14- Bis(ethyl)Homospermine." C.-Z. Chen, L. J. Hu, R. J. Bergeron, L. J. Marton, and D. F. Deen, Int. J. Radiat. Oncol. Biol. Phys., 29, 1041-1047 (1994).
122. "Role of Ribonucleotide Reductase in Inhibition of Mammalian Cell Growth by Potent Iron Chelators." S. Nyholm, G. J. Mann, A. G. Johansson, R. J. Bergeron, A. Graslund, and L. Thelander, J. Biol. Chem., 268, 26200-26205 (1993).
123. "Polyamine and Polyamine Analog Regulation of Spermidine/Spermine N1 Acetyltransferase in MALME-3M Human Melanoma Cells." M. Fogel-Petrovic, N. W. Shappell, R. J. Bergeron, and C. W. Porter, J. Biol. Chem., 268, 19118-19125 (1993).
124. "Total Synthesis of (+)-Hypusine and Its (2S,9S)-Diastereomer." R. J. Bergeron, M. X. B. Xia, and O. Phanstiel, IV, J. Org. Chem., 58, 6804-6806 (1993).
125. "The Desferrithiocin Pharmacophore." R. J. Bergeron, C. Z. Liu, J. S. McManis, M. X. B. Xia, S. E. Algee, and J. Wiegand, J. Med. Chem., 37 (10), 1411-1417 (1994).
126. "A Versatile Synthesis of Desferrioxamine." R.J. Bergeron, J. S. McManis, O. Phanstiel, IV, and J. R. T. Vinson, J. Org. Chem., 60(1), 109-114 (1995).
127. "Antiproliferative Properties of Polyamine Analogues: A Structure-Activity Study." R. J. Bergeron, J. S. McManis, C. Z. Liu, Y. Feng, W. R. Weimar, G. R. Luchetta, Q. Wu, J. Ortiz-Ocasio, J. R. T. Vinson, D. Kramer, and C. Porter, J. Med. Chem., 37(21), 3464-3476 (1994).
128. "Impact of Polyamine Analogues on the NMDA Receptor." R. J. Bergeron, W. R. Weimar, Q. Wu, J. K. Austin, Jr., and J. S. McManis, J. Med. Chem., 38, 425-428 (1995).
129. "An Investigation of Desferrithiocin Metabolism." R. J. Bergeron, M. Wollenweber, and J. Wiegand, J. Med. Chem., 37(18), 2889-2895 (1994).
130. "Macromolecular Self-Assembly of Diketopiperazine Tetrapeptides." R.J. Bergeron, O. Phanstiel, IV, G. W. Yao, S. Milstein, and W. R. Weimar, J. Amer. Chem. Soc., 116(19), 8479-8484 (1994).
131. "Design and Testing of Novel Cytotoxic Polyamine Analogues." H. S. Basu, L. J. Marton, M. Pellarin, D. F. Deen, J. S. McManis, C. Z. Liu, R. J. Bergeron, and B. G. Feuerstein, Cancer Res., 54, 6210-6214 (1994).
132. "Collateral Sensitivity of Human Melanoma Multidrug-resistant Variants to the Polyamine Analogue, N1,N11-Diethylnorspermine." C. W. Porter, B. Ganis, Y. Rustum, C. Wrzosek, D. L. Kramer, and R. J. Bergeron, Cancer Res., 54, 5917-5924 (1994).
133. "The Role of Charge in Polyamine Analogue Recognition." R. J. Bergeron, J. S. McManis, W. R. Weimar, K. Schreier, F. Gao, Q. Wu, J. Ortiz-Ocasio, G. R. Luchetta, C. Porter, and J. R. T. Vinson, J. Med. Chem., 38, 2278-2285 (1995).
134. "An Investigation of the Impact of Molecular Geometry upon Microcapsule Self- Assembly." R. J. Bergeron, G. W. Yao, G. W. Erdos, S. Milstein, F. Gao, W. R. Weimar, and O. Phanstiel, IV, J. Amer. Chem. Soc., 117, 6658-6665 (1995).
135. "Metabolism and Pharmacokinetics of N1, N11-Diethylnorspermine." R. J. Bergeron, W. R. Weimar, G. R. Luchetta, J. Wiegand, J. Perrin, K. Schreier, C. Porter, G. W. Yao, and H. Dimova, Drug Met. Dispos., 23(10), 1117-1125 (1995).
136. "The Impact of Polyamine Analogues on the Blood Pressure of Normotensive and Hypertensive Rats." R. J. Bergeron, J. Wiegand, C. A. Sninsky, and M. J. Katovich, Clin. Exper. Hypertension, 17(8), 1197-1217 (1995).
137. "Metabolism and Pharmacokinetics of N1,N14-Diethylhomospermine." R. J. Bergeron, W. R. Weimar, G. R. Luchetta, C. A. Sninsky, R. R. Streiff, and J. Wiegand, Drug Met. Dispos., 24(3), 334-343 (1996).
138. "Preclinical Antitumor Efficacy of the Polyamine Analogue N1,N11-Diethylnorspermine Administered by Multiple Injection or Continuous Infusion." R. J. Bernacki, E. J. Oberman, K. E. Seweryniak, A. Atwood, R. J. Bergeron, and C. W. Porter, Clin. Cancer Res., 1, 847-857 (1995).
139. "Metabolically Programmed Polyamine Analogue Antidiarrheals." R. J. Bergeron, G. W. Yao, H. Yao, W. R. Weimar, C. A. Sninsky, B. Raisler, Y. Feng, Q. Wu, and F. Gao, J. Med. Chem., 39(13), 2461-2471 (1996).
140. "Synthesis and Biological Evaluation of Naphthyldesferrithiocin Iron Chelators." R. J. Bergeron, J. Wiegand, M. Wollenweber, J. S. McManis, S. E. Algee, and K. Ratliff- Thompson, J. Med. Chem., 39(8), 1575-1581 (1996).
141. "Polyamine Analogue Regulation of NMDA MK-801 Binding: A Structure-Activity Study." R. J. Bergeron, W. R. Weimar, Q. Wu, Y. Feng, and J. S. McManis, J. Med. Chem., 39, 5257-5266 (1996).
142. "Total Synthesis of Rhizoferrin, An Iron Chelator." R. J. Bergeron, M. G. Xin, R. E. Smith, M. Wollenweber, J. S. McManis, C. Ludin, and K. A. Abboud, Tetrahedron, 53(2), 427-434 (1997).
143. "A Comparison of Structure-Activity Relationships between Spermidine and Spermine Analogue Antineoplastics." R. J. Bergeron, Y. Feng, W. R. Weimar, J. S. McManis, H. Dimova, C. Porter, B. Raisler, and O. Phanstiel, J. Med. Chem., 40(10), 1475-1494 (1997).
144. "The Development of a Hypusine Reagent for Peptide Synthesis." R. J. Bergeron, C. Ludin, R. Müller, R. E. Smith, and O. Phanstiel, IV, J. Org. Chem., 62(10), 3285-3290 (1997).
145. "Structural Basis for Differential Induction of Spermidine/Spermine N1-Acetyltransferase Activity by Novel Spermine Analogs." M. Fogel-Petrovic, D. L. Kramer, S. Vujcic, J. Miller, J. S. McManis, R. J. Bergeron, and C. Porter, Mol. Pharmacol., 52, 69-74 (1997).
146. "Human Prostatic Carcinoma Cell Lines Display Altered Regulation of Polyamine Transport in Response to Polyamine Analogs and Inhibitors." Z. Mi, D. L. Kramer, J. T. Miller, R. J. Bergeron, R. Bernacki, and C. W. Porter, Prostate, 34, 51-60 (1998).
147. "The Origin of the Differences in (R)-and (S)-Desferrithiocins: Iron-Clearing Properties." R. J. Bergeron, J. Wiegand, K. Ratliff-Thompson, and W. R. Weimar, Ann. N. Y. Acad. Sci., 850, 202-216 (1998).
148. "The Influence of Molecular Conformation Upon the Self-Assembly of Cyclohexane Diamide Diacids." R. J. Bergeron, G. W. Yao, G. W. Erdos, S. Milstein, F. Gao, J. Rocca, W. R. Weimar, H. L. Price, and O. Phanstiel, IV, Bioorg. Med. Chem., 5(11), 2049-2061 (1997).
149. "Effects of Novel Spermine Analogs on Cell Cycle Progression and Apoptosis in MALME-3M Human Melanoma Cells." D.L. Kramer, M. Fogel-Petrovic, P. Diegelman, J. M. Cooley, J. S. McManis, R. J. Bergeron, and C. Porter, Cancer Res., 57, 5521-5527 (1997).
150. "Polyamine Analogue Antiarrhythmics." R. J. Bergeron, J. Wiegand, W. R. Weimar, and P. S. Snyder, Pharm. Res., 38(5), 367-380 (1998).
151. "HBED: A Potential Alternative to Deferoxamine for Iron-Chelating Therapy." R. J. Bergeron, J. Wiegand, and G. M. Brittenham, Blood, 91(4), 1446-1452 (1998).
152. "Lysosomal Sequestration of Polyamine Analogs in Chinese Hamster Ovary Cells Resistant to the S-Adenosylmethionine Decarboxylase Inhibitor CGP-48664." D. L. Kramer, J. D. Black, H. Mett, R. J. Bergeron, and C. W. Porter, Cancer Res., 58, 3883-3890 (1998).
154. "Synthesis of Reagents for the Construction of Hypusine and Deoxyhypusine Peptides and their Application as Peptidic Antigens." R. J. Bergeron, W. R. Weimar, R. Müller, C. O. Zimmerman, B. H. McCosar, H. Yao, and R. E. Smith, J. Med. Chem., 41(20), 3888-3900 (1998).
155. "Effect of Polyamine Analogues on Hypusine Content in JURKAT T-Cells." R. J. Bergeron, W. R. Weimar, R. Müller, C. O. Zimmerman, B. H. McCosar, H. Yao, and R. E. Smith, J. Med. Chem., 41(20), 3901-3908 (1998).
156. "Desazadesmethyldesferrithiocin Analogues as Orally Effective Iron Chelators." R. J. Bergeron, J. Wiegand, W. R. Weimar, J. R. T. Vinson, J. Bussenius, G. W. Yao, and J. S. McManis, J. Med. Chem., 42, 95-108 (1999).
157. "HBED: The Continuing Development of A Potential Alternative to Deferoxamine for Iron-Chelating Therapy." R. J. Bergeron, J. Wiegand, and G. M. Brittenham, Blood, 93(1), 370-375 (1999).
Books
1. The Development of Iron Chelators for Clinical Use. R. J. Bergeron and G. M. Brittenham, Eds. CRC Press, Inc.: Boca Raton, FL (1994).
2. The Bioorganic Chemistry of Enzymatic Catalysis. M. L. Bender, R. J. Bergeron and M. Komiyama. John Wiley and Sons: New York, NY (1984).
