Raymond J Bergeron,
Eminent Scholar
Teaching Profile
Courses Taught
2009-2013
PHA7979 Advanced Research
2009-2013
PHA6934 Seminar in Medicinal Chemistry
2009-2013
PHA7980 Research for Doctoral Dissertation
2011-2013
PHA6910 Supervised Research
2010-2012
PHA6971 Masters Research
2010,2012
PHA6447 Drug Design
2009,2011
PHA5906 Research in Med Chem
Publications
2020
Targeting pheochromocytoma/paraganglioma with polyamine inhibitors.
Metabolism: clinical and experimental.
110
[DOI] 10.1016/j.metabol.2020.154297.
[PMID] 32562798.
2015
Metabolically programmed iron chelators.
Bioorganic & medicinal chemistry.
23(17):5954-71
[DOI] 10.1016/j.bmc.2015.06.059.
[PMID] 26231739.
2014
Desferrithiocin: a search for clinically effective iron chelators.
Journal of medicinal chemistry.
57(22):9259-91
[DOI] 10.1021/jm500828f.
[PMID] 25207964.
2012
Substituent effects on desferrithiocin and desferrithiocin analogue iron-clearing and toxicity profiles.
Journal of medicinal chemistry.
55(16):7090-103
[DOI] 10.1021/jm300509y.
[PMID] 22889170.
2011
Desferrithiocin analogue iron chelators: iron clearing efficiency, tissue distribution, and renal toxicity.
Biometals : an international journal on the role of metal ions in biology, biochemistry, and medicine.
24(2):239-58
[DOI] 10.1007/s10534-010-9389-y.
[PMID] 21103911.
2011
Synthesis of Heterobactins A and B and Nocardia Heterobactin.
Tetrahedron.
67(18):3163-3169
[PMID] 22539866.
2010
Design, Synthesis, and Testing of Polyamine Vectored Iron Chelators.
Synthesis.
2010(21):3631-3636
[PMID] 22013282.
2010
The impact of polyether chain length on the iron clearing efficiency and physiochemical properties of desferrithiocin analogues.
Journal of medicinal chemistry.
53(7):2843-53
[DOI] 10.1021/jm9018146.
[PMID] 20232803.
2009
Desferrithiocin analogue uranium decorporation agents.
International journal of radiation biology.
85(4):348-61
[DOI] 10.1080/09553000902781089.
[PMID] 19399680.
2009
Vibriobactin antibodies: a vaccine strategy.
Journal of medicinal chemistry.
52(12):3801-13
[DOI] 10.1021/jm900119q.
[PMID] 19492834.
2008
Desferrithiocin analogues and nephrotoxicity.
Journal of medicinal chemistry.
51(19):5993-6004
[DOI] 10.1021/jm8003398.
[PMID] 18788724.
2008
Design, synthesis, and testing of non-nephrotoxic desazadesferrithiocin polyether analogues.
Journal of medicinal chemistry.
51(13):3913-23
[DOI] 10.1021/jm800154m.
[PMID] 18533709.
2008
Medi 296-Bacterial Siderophore: New Versatile Synthesis and Stoichiometry of Vulnibactin
.
235
2008
Neurobiological and Clinical Effects of Combining Two Antidepressant Medications From the Start
International Journal of Neuropsychopharmacology.
11:9-10
2007
Impact of the 3,6,9-trioxadecyloxy group on desazadesferrithiocin analogue iron clearance and organ distribution.
Journal of medicinal chemistry.
50(14):3302-13
[PMID] 17564424.
2006
(S)-4,5-dihydro-2-(2-hydroxy-4-hydroxyphenyl)-4-methyl-4-thiazolecarboxylic acid polyethers: a solution to nephrotoxicity.
Journal of medicinal chemistry.
49(9):2772-83
[PMID] 16640338.
2006
The design, synthesis, and evaluation of organ-specific iron chelators.
Journal of medicinal chemistry.
49(24):7032-43
[PMID] 17125256.
2005
Partition-variant desferrithiocin analogues: organ targeting and increased iron clearance.
Journal of medicinal chemistry.
48(3):821-31
[PMID] 15689166.
2005
Polyamine-vectored iron chelators: the role of charge.
Journal of medicinal chemistry.
48(12):4120-37
[PMID] 15943485.
2005
Synthesis and biological evaluation of aminopolyamines.
Journal of medicinal chemistry.
48(9):3099-102
[PMID] 15857111.
2004
Comparison of iron chelator efficacy in iron-overloaded beagle dogs and monkeys (Cebus apella).
Comparative medicine.
54(6):664-72
[PMID] 15679265.
2003
Desferrithiocin analogue based hexacoordinate iron(III) chelators.
Journal of medicinal chemistry.
46(1):16-24
[PMID] 12502356.
2003
Iron chelation promoted by desazadesferrithiocin analogs: An enantioselective barrier.
Chirality.
15(7):593-9
[PMID] 12840823.
2003
Methoxylation of desazadesferrithiocin analogues: enhanced iron clearing efficiency.
Journal of medicinal chemistry.
46(8):1470-7
[PMID] 12672247.
2003
Polyamine-iron chelator conjugate.
Journal of medicinal chemistry.
46(25):5478-83
[PMID] 14640556.
2003
Prevention of acetic acid-induced colitis by desferrithiocin analogs in a rat model.
Digestive diseases and sciences.
48(2):399-407
[PMID] 12643622.
2002
HBED ligand: preclinical studies of a potential alternative to deferoxamine for treatment of chronic iron overload and acute iron poisoning.
Blood.
99(8):3019-26
[PMID] 11929795.
2002
Measurement of arsenic bioavailability in soil using a primate model.
Toxicological sciences : an official journal of the Society of Toxicology.
67(2):303-10
[PMID] 12011490.
2002
Structure-activity relationships among desazadesferrithiocin analogues.
Advances in experimental medicine and biology.
509:167-84
[PMID] 12572994.
2001
Control of irritable bowel syndrome with polyamine analogs: a structure-activity study.
Digestive diseases and sciences.
46(12):2615-23
[PMID] 11768250.
2001
Polyamine analogue antidiarrheals: a structure-activity study.
Journal of medicinal chemistry.
44(2):232-44
[PMID] 11170633.
2001
Significance of asymmetric sites in choosing siderophores as deferration agents.
Journal of medicinal chemistry.
44(15):2469-78
[PMID] 11448229.
2001
Synthesis and evaluation of hydroxylated polyamine analogues as antiproliferatives.
Journal of medicinal chemistry.
44(15):2451-9
[PMID] 11448227.
2000
Metabolism and pharmacokinetics of N1,N11-diethylnorspermine in a Cebus apella primate model.
Cancer research.
60(16):4433-9
[PMID] 10969789.
2000
Synthesis and evaluation of hydroxylated polyamine analogues as antiproliferatives.
Journal of medicinal chemistry.
43(2):224-35
[PMID] 10649978.
1999
Desazadesmethyldesferrithiocin analogues as orally effective iron chelators.
Journal of medicinal chemistry.
42(1):95-108
[PMID] 9888836.
1999
Effects of C-4 stereochemistry and C-4′ hydroxylation on the iron clearing efficiency and toxicity of desferrithiocin analogues.
Journal of medicinal chemistry.
42(13):2432-40
[PMID] 10395484.
1999
Evaluation of the desferrithiocin pharmacophore as a vector for hydroxamates.
Journal of medicinal chemistry.
42(15):2881-6
[PMID] 10425097.
1999
HBED: the continuing development of a potential alternative to deferoxamine for iron-chelating therapy.
Blood.
93(1):370-5
[PMID] 9864183.
1999
Pharmacokinetics of orally administered desferrithiocin analogs in cebus apella primates.
Drug metabolism and disposition: the biological fate of chemicals.
27(12):1496-8
[PMID] 10570032.
1999
Polyamine analogue induction of the p53-p21WAF1/CIP1-Rb pathway and G1 arrest in human melanoma cells.
Cancer research.
59(6):1278-86
[PMID] 10096560.
1998
Effect of polyamine analogues on hypusine content in JURKAT T-cells.
Journal of medicinal chemistry.
41(20):3901-8
[PMID] 9748365.
1998
HBED: A potential alternative to deferoxamine for iron-chelating therapy.
Blood.
91(4):1446-52
[PMID] 9454776.
1998
Human prostatic carcinoma cell lines display altered regulation of polyamine transport in response to polyamine analogs and inhibitors.
The Prostate.
34(1):51-60
[PMID] 9428388.
1998
Lysosomal sequestration of polyamine analogues in Chinese hamster ovary cells resistant to the S-adenosylmethionine decarboxylase inhibitor, CGP-48664.
Cancer research.
58(17):3883-90
[PMID] 9731498.
1998
Polyamine analogue antiarrhythmics.
Pharmacological research.
38(5):367-80
[PMID] 9806817.
1998
Synthesis of reagents for the construction of hypusine and deoxyhypusine peptides and their application as peptidic antigens.
Journal of medicinal chemistry.
41(20):3888-900
[PMID] 9748364.
1998
The origin of the differences in (R)- and (S)-desmethyldesferrithiocin. Iron-clearing properties.
Annals of the New York Academy of Sciences.
850:202-16
[PMID] 9668541.
1997
A comparison of structure-activity relationships between spermidine and spermine analogue antineoplastics.
Journal of medicinal chemistry.
40(10):1475-94
[PMID] 9154970.
1997
Development of a Hypusine Reagent for Peptide Synthesis.
The Journal of organic chemistry.
62(10):3285-3290
[PMID] 11671715.
1997
Effects of novel spermine analogues on cell cycle progression and apoptosis in MALME-3M human melanoma cells.
Cancer research.
57(24):5521-7
[PMID] 9407962.
1997
Structural basis for differential induction of spermidine/spermine N1-acetyltransferase activity by novel spermine analogs.
Molecular pharmacology.
52(1):69-74
[PMID] 9224814.
1997
The influence of molecular conformation upon the self-assembly of cyclohexane diamide diacids.
Bioorganic & medicinal chemistry.
5(11):2049-61
[PMID] 9416422.
1996
Metabolically programmed polyamine analogue antidiarrheals.
Journal of medicinal chemistry.
39(13):2461-71
[PMID] 8691443.
1996
Metabolism and pharmacokinetics of N1,N14-diethylhomospermine.
Drug metabolism and disposition: the biological fate of chemicals.
24(3):334-43
[PMID] 8820425.
1996
Polyamine analogue regulation of NMDA MK-801 binding: a structure-activity study.
Journal of medicinal chemistry.
39(26):5257-66
[PMID] 8978854.
1996
Synthesis and biological evaluation of naphthyldesferrithiocin iron chelators.
Journal of medicinal chemistry.
39(8):1575-81
[PMID] 8648596.
1995
Impact of polyamine analogues on the NMDA receptor.
Journal of medicinal chemistry.
38(3):425-8
[PMID] 7853334.
1995
Metabolism and pharmacokinetics of N1,N11-diethylnorspermine.
Drug metabolism and disposition: the biological fate of chemicals.
23(10):1117-25
[PMID] 8654201.
1995
Preclinical antitumor efficacy of the polyamine analogue N1, N11-diethylnorspermine administered by multiple injection or continuous infusion.
Clinical cancer research : an official journal of the American Association for Cancer Research.
1(8):847-57
[PMID] 9816054.
1995
The impact of polyamine analogues on the blood pressure of normotensive and hypertensive rats.
Clinical and experimental hypertension (New York, N.Y. : 1993).
17(8):1197-217
[PMID] 8563697.
1995
The role of charge in polyamine analogue recognition.
Journal of medicinal chemistry.
38(13):2278-85
[PMID] 7608892.
1994
An investigation of desferrithiocin metabolism.
Journal of medicinal chemistry.
37(18):2889-95
[PMID] 8071936.
1994
Antiproliferative properties of polyamine analogues: a structure-activity study.
Journal of medicinal chemistry.
37(21):3464-76
[PMID] 7932575.
1994
Collateral sensitivity of human melanoma multidrug-resistant variants to the polyamine analogue, N1,N11-diethylnorspermine.
Cancer research.
54(22):5917-24
[PMID] 7954423.
1994
Design and testing of novel cytotoxic polyamine analogues.
Cancer research.
54(23):6210-4
[PMID] 7954468.
1994
Radiopotentiation of human brain tumor cells by the spermine analog N1,N14-bis(ethyl)homospermine.
International journal of radiation oncology, biology, physics.
29(5):1041-7
[PMID] 8083073.
1994
The desferrithiocin pharmacophore.
Journal of medicinal chemistry.
37(10):1411-7
[PMID] 8182699.
1993
A comparative study of the iron-clearing properties of desferrithiocin analogues with desferrioxamine B in a Cebus monkey model.
Blood.
81(8):2166-73
[PMID] 8471775.
1993
Antitumor activity of N1,N11-bis(ethyl)norspermine against human melanoma xenografts and possible biochemical correlates of drug action.
Cancer research.
53(3):581-6
[PMID] 8425191.
1993
Effects of diethyl spermine analogues in human bladder cancer cell lines in culture.
The Journal of urology.
150(4):1293-7
[PMID] 8371417.
1993
Growth inhibition of hormone-responsive and -resistant human breast cancer cells in culture by N1, N12-bis(ethyl)spermine.
Cancer research.
53(9):2071-5
[PMID] 8481909.
1993
Investigations of the mechanism by which mammalian cell growth is inhibited by N1N12-bis(ethyl)spermine.
The Biochemical journal.
291 ( Pt 1)(Pt 1):131-7
[PMID] 8471032.
1993
Polyamine and polyamine analog regulation of spermidine/spermine N1-acetyltransferase in MALME-3M human melanoma cells.
The Journal of biological chemistry.
268(25):19118-25
[PMID] 8360194.
1993
Regulation of polyamine transport by polyamines and polyamine analogs.
Journal of cellular physiology.
155(2):399-407
[PMID] 8482732.
1993
Role of ribonucleotide reductase in inhibition of mammalian cell growth by potent iron chelators.
The Journal of biological chemistry.
268(35):26200-5
[PMID] 8253740.
1992
A comparison of the iron-clearing properties of 1,2-dimethyl-3-hydroxypyrid-4-one, 1,2-diethyl-3-hydroxypyrid-4-one, and deferoxamine.
Blood.
79(7):1882-90
[PMID] 1558978.
1992
Antitumor activity of N,N’-bis(ethyl)spermine homologues against human MALME-3 melanoma xenografts.
Cancer research.
52(9):2424-30
[PMID] 1568212.
1992
Antitumor effects of N-alkylated polyamine analogues in human pancreatic adenocarcinoma models.
Cancer chemotherapy and pharmacology.
30(3):179-82
[PMID] 1628365.
1992
Differential effects of the spermine analog, N1, N12-bis(ethyl)-spermine, on polyamine metabolism and cell growth in human melanoma cell lines and melanocytes.
Anticancer research.
12(4):1083-9
[PMID] 1503400.
1992
Regulatory and antiproliferative effects of N-alkylated polyamine analogues in human and hamster pancreatic adenocarcinoma cell lines.
Cancer chemotherapy and pharmacology.
30(3):183-8
[PMID] 1628366.
1992
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.
Cancer research.
52(19):5359-63
[PMID] 1327507.
1992
Structural alterations in desferrioxamine compatible with iron clearance in animals.
Journal of medicinal chemistry.
35(25):4739-44
[PMID] 1469701.
1991
Characterization of human spermidine/spermine N1-acetyltransferase purified from cultured melanoma cells.
Archives of biochemistry and biophysics.
284(2):238-44
[PMID] 1989509.
1991
Correlations between polyamine analogue-induced increases in spermidine/spermine N1-acetyltransferase activity, polyamine pool depletion, and growth inhibition in human melanoma cell lines.
Cancer research.
51(14):3715-20
[PMID] 2065327.
1991
Evaluation of desferrithiocin and its synthetic analogues as orally effective iron chelators.
Journal of medicinal chemistry.
34(7):2072-8
[PMID] 2066978.
1991
Increase in spermine content coordinated with siderophore production in Paracoccus denitrificans.
Journal of bacteriology.
173(7):2238-43
[PMID] 1826103.
1991
Selective cellular depletion of mitochondrial DNA by the polyamine analog N1,N12-bis(ethyl)spermine and its relationship to polyamine structure and function.
Molecular pharmacology.
39(4):487-94
[PMID] 2017149.
1991
Synthesis and biological evaluation of hydroxamate-based iron chelators.
Journal of medicinal chemistry.
34(11):3182-7
[PMID] 1956036.
1990
A comparative evaluation of iron clearance models.
Annals of the New York Academy of Sciences.
612:378-93
[PMID] 2127168.
1990
Combined regulation of ornithine and S-adenosylmethionine decarboxylases by spermine and the spermine analogue N1 N12-bis(ethyl)spermine.
The Biochemical journal.
268(1):207-12
[PMID] 2344358.
1990
Effect of N1,N14-bis(ethyl)homospermine on the growth of U-87 MG and SF-126 human brain tumor cells.
Cancer research.
50(11):3137-40
[PMID] 2334909.
1990
Induction of spermidine/spermine N1-acetyltransferase activity in Chinese-hamster ovary cells by N1N11-bis(ethyl)norspermine (corrected) and related compounds.
The Biochemical journal.
267(2):331-8
[PMID] 2334396.
1990
Kinetics of iron acquisition from ferric siderophores by Paracoccus denitrificans.
Journal of bacteriology.
172(5):2650-7
[PMID] 2185228.
1989
Correlation between the effects of polyamine analogues on DNA conformation and cell growth.
Cancer research.
49(20):5591-7
[PMID] 2507131.
1989
Differential induction of spermidine/spermine N1-acetyltransferase in human lung cancer cells by the bis(ethyl)polyamine analogues.
Cancer research.
49(14):3829-33
[PMID] 2544259.
1989
Differential response to treatment with the bis(ethyl)polyamine analogues between human small cell lung carcinoma and undifferentiated large cell lung carcinoma in culture.
Cancer research.
49(3):639-43
[PMID] 2535963.
1989
Effect of N1,N12-bis(ethyl)spermine and related compounds on growth and polyamine acetylation, content, and excretion in human colon tumor cells.
The Journal of biological chemistry.
264(20):11744-9
[PMID] 2745415.
1989
Major increases in spermidine/spermine-N1-acetyltransferase activity by spermine analogues and their relationship to polyamine depletion and growth inhibition in L1210 cells.
Cancer research.
49(22):6226-31
[PMID] 2804970.
1989
Role of the methylene backbone in the antiproliferative activity of polyamine analogues on L1210 cells.
Cancer research.
49(11):2959-64
[PMID] 2720656.
1989
Structure-function correlations of polyamine analog-induced increases in spermidine/spermine acetyltransferase activity.
Biochemical pharmacology.
38(9):1435-42
[PMID] 2497746.
1988
Control of ornithine decarboxylase activity in alpha-difluoromethylornithine-resistant L1210 cells by polyamines and synthetic analogues.
The Journal of biological chemistry.
263(22):11008-14
[PMID] 3134356.
1988
Demonstration of ferric L-parabactin-binding activity in the outer membrane of Paracoccus denitrificans.
Journal of bacteriology.
170(8):3711-7
[PMID] 3403511.
1988
Enzyme regulation as an approach to interference with polyamine biosynthesis–an alternative to enzyme inhibition.
Advances in enzyme regulation.
27:57-79
[PMID] 3250233.
1988
Modulation of polyamine biosynthesis and transport by oncogene transfection.
Biochemical and biophysical research communications.
157(1):264-70
[PMID] 3143363.
1988
Regulation of polyamine biosynthetic activity by spermidine and spermine analogs–a novel antiproliferative strategy.
Advances in experimental medicine and biology.
250:677-90
[PMID] 3076344.
1988
Selective regulation of S-adenosylmethionine decarboxylase activity by the spermine analogue 6-spermyne.
The Biochemical journal.
254(2):337-42
[PMID] 3178763.
1988
Synthetic polyamine analogues as antineoplastics.
Journal of medicinal chemistry.
31(6):1183-90
[PMID] 3373487.
1987
Microbial iron chelator-induced cell cycle synchronization in L1210 cells: potential in combination chemotherapy.
Cancer research.
47(22):6010-6
[PMID] 3664504.
1987
Regulation of ornithine decarboxylase activity by spermidine and the spermidine analogue N1N8-bis(ethyl)spermidine.
The Biochemical journal.
242(2):433-40
[PMID] 3036091.
1987
Relative abilities of bis(ethyl) derivatives of putrescine, spermidine, and spermine to regulate polyamine biosynthesis and inhibit L1210 leukemia cell growth.
Cancer research.
47(11):2821-5
[PMID] 3567905.
1987
Structural determinants of spermidine-DNA interactions.
Biopolymers.
26(5):691-703
[PMID] 3593890.
1986
Comparison and characterization of growth inhibition in L1210 cells by alpha-difluoromethylornithine, an inhibitor of ornithine decarboxylase, and N1,N8-bis(ethyl)spermidine, an apparent regulator of the enzyme.
Cancer research.
46(12 Pt 1):6279-85
[PMID] 3096560.
1986
Effects of the Vibrio cholerae siderophore vibriobactin on the growth characteristics of L1210 cells.
Biochemical and biophysical research communications.
136(1):273-80
[PMID] 3707576.
1985
Biological properties of N4- and N1,N8-spermidine derivatives in cultured L1210 leukemia cells.
Cancer research.
45(5):2050-7
[PMID] 3921235.
1985
Characterization of L1210 cell growth inhibition by the bacterial iron chelators parabactin and compound II.
Cancer research.
45(10):4754-9
[PMID] 4027962.
1985
Influence of iron on in vivo proliferation and lethality of L1210 cells.
The Journal of nutrition.
115(3):369-74
[PMID] 3973748.
1985
Mechanism and stereospecificity of the parabactin-mediated iron-transport system in Paracoccus denitrificans.
The Journal of biological chemistry.
260(13):7936-44
[PMID] 4008483.
1984
Aliphatic chain length specificity of the polyamine transport system in ascites L1210 leukemia cells.
Cancer research.
44(1):126-8
[PMID] 6690029.
1984
Antineoplastic and antiherpetic activity of spermidine catecholamide iron chelators.
Biochemical and biophysical research communications.
121(3):848-54
[PMID] 6331431.
1984
Treatment with alpha-difluoromethylornithine plus a spermidine analog leads to spermine depletion and growth inhibition in cultured L1210 leukemia cells.
Journal of cellular physiology.
121(3):476-82
[PMID] 6438117.
1983
Bacteriostatic and fungostatic action of catecholamide iron chelators.
Antimicrobial agents and chemotherapy.
24(5):725-30
[PMID] 6419673.
1983
Spermidine requirement for cell proliferation in eukaryotic cells: structural specificity and quantitation.
Science (New York, N.Y.).
219(4588):1083-5
[PMID] 6823570.
1982
Biological properties of N4-spermidine derivatives and their potential in anticancer chemotherapy.
Cancer research.
42(10):4072-8
[PMID] 7105005.
1980
Synthesis, absorption, and toxicity of N1,N8-bis(2,3-dihydroxybenzoyl)spermidine, a potent iron chelator.
Journal of medicinal chemistry.
23(10):1130-3
[PMID] 7420358.
Grants
Mar 2010
– May 2016
Iron Chelators Predicated on Desferrithiocin.
Role: Principal Investigator
Funding: NATL INST OF HLTH NIDDK
Contact Details
Phones:
- Business:
- (352) 273-7725
Emails:
- Business:
- rayb@ufl.edu
Addresses:
- Business Mailing:
-
PO Box 100485
GAINESVILLE FL 32610 - Business Street:
-
P6-04 JHMHC
GAINESVILLE FL 32610