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Publications et Brevets de l’équipe « Nucléosides et Effecteurs Phosphorylés »

depuis 2006

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Publications (journaux à comité de lecture)


« Prodrugs of Nucleoside 5’-Monophosphate Analogues : Overview of the Recent Literature Concerning their Synthesis and Applications » B. Roy, V. Navarro, S. Peyrottes ; Curr. Med. Chem., accepté en novembre 2022


« Synthesis of N-methylene phosphonate aziridines : reaction scope and mechanistic insights » Cheviet T., Gonzales I., and Peyrottes S. ; New Journal of Chemistry (2022), 46 (14), 6453-6460

« Supported Synthesis of Adenosine Nucleotides and Derivatives on a Benzene-Centered Tripodal Soluble Support » Appy, L., Peyrottes, S. and Roy, B. ; European Journal of Organic Chemistry (2022),e202100544

« Discovery of an L-like Configuration for 3’-Fluoro-5’-norcarbonucleoside Phosphonates as Potent Anti-HIV Agents » P.-Y. Geant, M. Kaci, J.-P. Uttaro, C. Périgaud, C. Mathé ; ChemMedChem 2022, 17, e202200377

« Mononucleoside phosphorodithiolates as mononucleotide prodrugs » N. Schlienger, I. Lefebvre, A.-M. Aubertin, S. Peyrottes, C. Périgaud ; European Journal of Medicinal Chemistry, (2022), 113914,

« Cytotoxic and Antitumoral Activity of N-(9H-purin-6-yl) Benzamide Derivatives and Related Water-soluble Prodrugs » E. Cros-Perrial, S. Saulnier, M. Z. Raza1, R. Charmelot, D. Egron, C. Dumontet, L. Chaloin, S. Peyrottes and L. P. Jordheim ;
Current Molecular Pharmacology (2022), 15(6), 883-894.

« Synthesis and Studies of Potential Inhibitors of CD73 Based on a Triazole Scaffold »
F. Grosjean, E. Cros-Perrial, A. Braka, J.-P. Uttaro, L. Chaloin, L. P. Jordheim, S. Peyrottes, C. Mathé ; European Journal of Organic Chemistry (2022),e202101175


« Addition to “Reactions : An Innovative and Fun Hybrid Game to Engage the Students Reviewing Organic Reactions in the Classroom : Using the Game Remotely during the COVID-19 Pandemic » J. N. da Silva Júnior, M. A. Sousa Lima, U. Silva de Sousa, D. M. do Nascimento, A. J. M. L. Junior, K. B. Vega, B. Roy, and J.-Y. Winum ; Journal of Chemical Education, 2021, 98 (8), 2735–2737.

« 2’-Derivatisation of 3’-C-Methyl Pyrimidine Nucleosides » S. Couturier, S.Peyrottes, C. Périgaud ; European Journal of Organic Chemistry, 2021, 29, 4007-4014.

« An original pronucleotide strategy for the simultaneous delivery of two bioactive drugs » A. L. Villard, A. M. Aubertin, S. Peyrottes, C. Perigaud ; European Journal of Medicinal Chemistry, 2021, 216, 113315.

« Synthesis of Aminomethylene-gem-bisphosphonates Containing an Aziridine Motif : Studies of the Reaction Scope and Insight into the Mechanism » T. Cheviet, S.Peyrottes ; Journal of Organic Chemistry, 2021, 86, 4, 3107–3119.

« 4-Substituted-1,2,3-triazolo nucleotide analogues as CD73 inhibitors, their synthesis, in vitro screening, kinetic and in silico studies » R. Ghoteimi, A. Brakab, C. Rodriguez, E. Cros-Perrial, V.T. Nguyen, J.-P. Uttaro, C. Mathé, L. Chaloin, C. Ménétrier-Caux, L. P. Jordheim, S. Peyrottes, Bioorganic Chemistry, 2021, 107, 104577.

« Synthesis and Studies of Potential Inhibitors of CD73 Based on a Triazole Scaffold » F. Grosjean, E. Cros-Perrial, A. Braka, J.-P. Uttaro, L. Chaloin, L. P. Jordheim, S. Peyrottes, C. Mathé, European Journal of Organic Chemistry, 2021.

« Alternative synthetic approaches for nucleotides and derivatives » L. Appy, A. Depaix, X. Bantreil, F. Lamaty, S. Peyrottes, B. Roy, Phosphorus, Sulfur, and Silicon and the Related Elements, 2021.

Presentations 2021

Triazolo nucleotide analogues as New Chemotype for CD73 inhibition
Rayane Ghoteimi / Oral Communication IS3NA congress. August 26-27, 2021

Beta-substituted acyclic nucleoside phosphonates as potent antimalarials - Triazolo nucleotide analogues as New Chemotype for CD73 inhibition
Thomas Cheviet / Poster presentation IS3NA congress. August 26-27, 2021.


« Synthesis and Antiviral Evaluation of 3′-Fluoro-5′-norcarbocyclic Nucleoside Phosphonates Bearing Uracil and Cytosine as Potential Antiviral Agents » P.-Y. Géant,
J.-P. Uttaro, C. Périgaud, C. Mathé ; Molecules, 25 (16), 3708 (2020).

« A synergistic synthetic and computational insights towards anomerization of N-nitro pyrimidine nucleosides using fluorinating agents » A. Khalil, I. Bayach, C. Mathé ; Journal of Fluorine Chemistry, 233, 109504 (2020).

« β-Hydroxy- and β-Aminophosphonate Acyclonucleosides as Potent Inhibitors of Plasmodium falciparum Growth » T. Cheviet, S. Wein, G. Bourchenin, M. Lagacherie, C. Périgaud, R. Cerdan, S.Peyrottes ; Journal of Medicinal Chemistry 63, 8069−8087,(2020).

« 2-(Substituted amino)-8-azachromones from 4,6-Diaryl-2-pyridones : a Synthetic Strategy toward Compounds of Broad Structural Diversity » S. Saulnier, R. Ghoteimi, C. Mathé, S. Peyrottes, J.-P. Uttaro ; Journal of Organic Chemistry, 85,11778–11793 (2020).

« Intracellular anabolism of 5-fluorouracil and incorporation in nucleic acids based on a LC-HRMS method », C. Machon, F. Catez, N. Dalla Venezia, F. Vanhalle, L. Guyot, A. Vincent, M. Garcia, B. Roy, J.-J. Diaz, J. Guitton ; Journal of Pharmaceutical Analysis (2020).

« Reactions : An Innovative and Fun Hybrid Game to Engage the Students Reviewing Organic Reactions in the Classroom », J. Nunes da Silva Júnior, M. A. S. Lima, U. Silva de Sousa, D. Macedo do Nascimento, A. J. M. Leite Junior, K. B. Vega, B. Roy, J.-Y. Winum ; Journal of Chemical Education. 97 (3), 749-753 (2020).


« Synthetic strategies for dinucleotides synthesis », L. Appy, C. Chardet, S. Peyrottes, B. Roy ; Molecules, 24, 4334 (2019).
doi : 10.3390/molecules24234334

« Lead optimization and biological evaluation of fragment-based cN-II inhibitors », R. Guillon, R. Rahimova, Preeti, D. Egron, S. Rouanet, C. Dumontet, N. Aghajari, L.P. Jordheim, L. Chaloin, S. Peyrottes ; European Journal of Medicinal Chemistry, 168, 28-44 (2019).
doi : 10.1016/j.ejmech.2019.02.040

« Synthesis and Antiviral Evaluation of 3 ’-Fluoro-4 ’-modified-5 ’-norcarbocyclic Nucleoside Phosphonates », P.Y. Géant, M. Kaci, J.P. Uttaro, C. Périgaud, C. Mathé ; ChemMedChem, 14 (5), 522-526 (2019).
doi : 10.1002/cmdc.201800804

« Plasmodium Purine Metabolism and Its Inhibition by Nucleoside and Nucleotide Analogues », T. Cheviet, I. Lefebvre-Tournier, S. Wein, S. Peyrottes ; Journal of Medicinal Chemistry, 62 (18), 8365-8391 (2019).
doi : 10.1021/acs.jmedchem.9b00182

« Synthesis of Substituted 5 ’-Aminoadenosine Derivatives and Evaluation of Their Inhibitory Potential toward CD73 », R. Ghoteimi, V.T. Nguyen,R. Rahimova, S., F. Grosjean, E. Cros-Perrial, J.-P.Uttaro, C. Mathe, L. Chaloin, L.P. Jordheim, S. Peyrottes ; ChemMedChem, 14 (15), 1431-1443 (2019).
doi : 10.1002/cmdc.201900348

« Straightforward Ball‐Milling Access to Dinucleoside 5’,5’‐Polyphosphates Through Phosphorimidazolide Intermediates », L. Appy, A. Depaix, X. Bantreil, F. Lamaty, S. Peyrottes, B. Roy ; Chemistry - A European Journal, 25 (10), 2477-2481 (2019).
doi : 10.1002/chem.201805924


“CD73 inhibition by purine cytotoxic nucleoside analogue-based diphosphonates”, C. Dumontet, S. Peyrottes, C ; Rabeson, E. Cross-Perrial, P.Y. Géant, L. Chaloin, L.P. Jordheim ; European Journal of Medicinal Chemistry, 157, 1051-1055 (2018). . doi : 10.1016/j.ejmech.2018.08.035

“Contribution of the precursors and interplay of the pathways in the phospholipid metabolism of the malaria parasite”, S. Wein, S. Ghezal, C. Bure, M. Maynadier, C. Périgaud, H.J. Vial, I. Lefebvre-Tournier, K. Wengelnik, R. Cerdan ; Journal of Lipid Research, 59 (8), 1461-1471 (2018). doi : 10.1194/jlr.M085589

“Rapid Synthesis of carbonucleoside phosphonate analogues as potential antiviral agents via a hydrophosphonylation reaction of ethynyl carbocyclic precursors”, B. Sidi Mohamed, C. Périgaud, S. Peyrottes, J.-P. Uttaro, C. Mathé ; New Journal of Chemistry, 42 (2), 974-979 (2018). doi : 10.1039/C7NJ03991C

“Identification of allosteric inhibitors of the ecto-5’-nucleotidase (CD73) targeting the dimer interface”, R. Rahimova, S. Fontanel, C. Lionne, L.P. Jordheim, S. Peyrottes, L. Chaloin, PLOS Computational Biology, 14(1) : e1005943 .doi : 10.1371/journal.pcbi.1005943

“Synthesis of tRNA analogues containing a terminal ribose locked in the South conformation to study tRNA-dependent enzymes”, L. Iannazzo, M. Fonvieille, E. Braud, H. Hrebabecky, E. Prochazkova, R. Nencka, C. Mathé, M. Arthur, M. Etheve-Quelquejeu ; Organic & Biomolecular Chemistry, 16 (11), 1903-1911 (2018). doi : 10.1039/C8OB00019K

“Synthesis of 3′-halo-5′-norcarbocyclic nucleoside phosphonates as potent anti- HIV agents”, N. Hamon, M. Kaci, J.-P. Uttaro, C. Périgaud, C. Mathé ; European Journal of Medicinal Chemistry, 150, 642-654 (2018). doi : 10.1016/j.ejmech.2018.03.038

« New insights for the preparation of cytidine containing nucleotides using a soluble ether-linked polyethylene glycol support », A. Depaix, J.-Y. Puy, B. Roy, S. Peyrottes ; New Journal of Chemistry, 42, 16441-16445 (2018). doi : 10.1039/C8NJ03753A

« Synthesis and substrate properties towards HIV-1 reverse transcriptase of new diphosphate analogues of 9-[(2-phosphonomethoxy)ethyl]adenine », W.H.G. Laux, S. Priet, K. Alvarez, S. Peyrottes, C. Périgaud ; Antiviral Chemistry & Chemotherapy, 26, 1-8 (2018). doi : 10.1177/2040206618757636.


« Determination and quantification of intracellular fludarabine triphosphate, cladribine triphosphate and clofarabine triphosphate by LC-MS/MS in human cancer cells », J.-Y. puy, L. P. Jordheim, E. Cros-Perrial, C. Dumontet, S. Peyrottes, I. Lefebvre-Tournier ; Journal of Chromatography B, 1053, 101-110 (2017).

« Water medium synthesis of nucleoside 5’-polyphosphates », A. Depaix, S. Peyrottes, B. Roy ; Current Protocols in Nucleic Acid Chemistry, 69, 13.16.1-13.16.11 (2017). doi : 10.1002/cpnc.30

« Evidence that oxidative dephosphorylation by the nonheme Fe(II), a-ketoglutarate : UMP oxygenase occurs by stereospecific hydroxylation », A. Goswami, X. Liu, W. Cai, T. P. Wyche, T. S. Bugni, M. Meurillon, S. Peyrottes, C. Perigaud, K. Nonaka, J. Rohr, S. G. Van Lanen, FEBS Letters 591 (3), 468–478 (2017). doi:10.1002/1873-3468.12554.

“Revaluation of biomass-derived furfuryl alcohol derivatives for the synthesis of carbocyclic nucleoside phosphonate analogues”, B. Sidi Mohamed, C. Périgaud, C. Mathé ; Beilstein Journal of Organic Chemistry ; 13, 251-256 (2017). doi:10.3762/bjoc.13.28.

« One-pot synthesis of nucleotides and conjugates in aqueous medium », A. Depaix, S. Peyrottes, B. Roy ; European Journal of Organic Chemistry, 2, 241-245 (2017). doi : 10.1002/ejoc.201601299.

“An eco-friendly and efficient photoinduced coupling of alkenes and alkynes with H-phosphinates and other P(O)H derivatives under free-radical conditions”, P.-Y. Géant, J.-P. Uttaro, S. Peyrottes, C. Mathé, European Journal of Organic Chemistry, 26, 3850-3855 (2017). doi : 10.1002/ejoc.201700584.

“The cytosolic 5’-nucleotidase cN-II lowers the adaptability to glucose deprivation in human breast cancer cells.” G. Bricard, O. Cadassou, L-E Cassagnes, E. Cros-Perrial, L. Payen-Gay, J.-Y. Puy, I. Lefebvre-Tournier, M. Grazia-Tozzi, C. Dumontet, L. Jordheim, Oncotarget, 8 (40), 67380-67393 (2017). doi : 10.18632/oncotarget.18653.
“Vc9Vd2 T cell activation by strongly agonistic nucleotidic phosphoantigens.” M. Moulin, J. AlguacilL, S. Gu, A. Mehtougui, E.J. Adams, S. Peyrottes, E. Champagne, Cellular and Molecular Life Sciences, 74 (23), 4353-4367 (2017). doi:10.1007/s00018-017-2583-0.

“The discovery of IDX21437 : Design, synthesis and antiviral evaluation of 2’-alpha-chloro-2’-béta-C-methyl branched uridine pronucleotides as potent liver-targeted HCV polymerase inhibitors.” F-R. Alexandre, E. Badaroux, J. P. Bilello, S. Bot, T. Bouisset, G. Brandt, S. Cappelle, C. Chapron, D. Chaves, T. Convard, C. Counor, D. Da Costa, D. Dukhan, M. Gay, G. Gosselin, J.-F. Grffon, K. Gupta, B. Hernandez-Santiago, M. La Colla, M-P. Lioure, J. Milhau, J-L. Paparin, J. Peyronnet, C. Parsy, C. Pierra Rouvière, H. Rahali, R. Rahali, A. Salanson, M. Seifer, I. Serra, D. Standring, D. Surleraux, C. B. Dousson, Bioorganic & Medicinal Chemistry Letters, 27 (18), 4323-4330 (2017). doi : 10.1016/j.bmcl.2017.08.029 0.


“Intracellular Metabolism of Nucleoside/Nucleotide Analogues : a Bottleneck to Reach Active Drugs on HIV Reverse Transcriptase”, A. Varga, C. Lionne, B. Roy, Current Drug Metabolism, 17 (3), 237-252 (2016).

“Aminobisphosphonates Synergize with Human Cytomegalovirus To Activate the Antiviral Activity of Vg9Vd2 Cells”, C. Daguzan, M. Moulin, H. Kulyk-Barbier, C. Davrinche, S. Peyrottes, E. Champagne, Journal of Immunology, 196 (5), 2219-2229 (2016).

“Probing the reactivity of H-phosphonate derivatives for the hydrophosphonylation of various alkenes and alkynes under free-radical conditions”, P.-Y. Géant, B. Sidi Mohamed, C. Périgaud, S. Peyrottes, J.-P. Uttaro, C. Mathé ; New Journal of Chemistry, 40 (6), 5318-5324 (2016).

“Exploring synthetic pathways for nucleosidic derivatives of potent phosphoantigens”, J. Alguacil, D. Reyes, Y. Aubin, B. Roy, C. Périgaud, E. Champagne, S. Peyrottes, New Journal of Chemistry, 40 (7), 6046-6052 (2016).

“Beta-hydroxyphosphonate ribonucleoside analogues derived from 4-substituted-1,2,3-triazoles as IMP/GMP mimics : synthesis and biological evaluation”, T. Nguyen Van, A. Hospital, C. Lionne, L.P. Jordheim, C. Dumontet, C. Périgaud, L. Chaloin, S. Peyrottes, Beilstein Journal of Organic Chemistry, 12, 1476-1486 (2016).

“Recent Trends in Nucleotide Synthesis”, B. Roy, A. Depaix, C. Périgaud, S. Peyrottes, Chemical Reviews, 116 (14), 7854-7897 (2016).


PCT/WO2015/049447(A1), 09.04.2015 : « Inhibiteurs de 5’-Nucléotidases et leurs utilisations thérapeutiques », Inventeur : L. CHALOIN, S. PEYROTTES, C. LIONNE, Z. MARTON, D. EGRON, R. GUILLON, C. PERIGAUD, C. DUMONTET, L. JORDHEIM, I. KRIMM, (déposé le 1er octobre 2013, N° 1359472).

“Identification of Noncompetitive Inhibitors of Cytosolic 5 ’-Nucleotidase II Using a Fragment-Based Approach”, Z. MARTON, R. GUILLON, I. KRIMM, Krimm, PREETI, R.RAHIMOVA, D. EGRON, LP JORDHEIM, N. AGHAJARI, C. DUMONTET, C. PERIGAUD, C. LIONNE, S. PEYROTTES, L. CHALOIN, Journal of Medicinal Chemistry, 58 (24), 9680-9696.

“Determination of the enzymatic activity of cytosolic 5 ’-nucleotidase cN-II in cancer cells : development of a simple analytical method and related cell line models”, LP JORDHEIM, JY PUY, E. CROS-PERRIAL, S. PEYROTTES, I. LEFEBVRE, C. PERIGAUD, C. DUMONTET, Analytical and Bioanalytical Chemistry, 407 (19), 5747-5758.


“Synthesis of unnatural 2-and 3-deoxyfuranose analogues”, B. DAYDE, C. PIERRA, G. GOSSELIN, D. SURLERAUX, A.T. ILAGOUMA, A. Van DER LEE, J.N. VOLLE, D. VIRIEUX, J.-L. PIRAT, Tetrahedron Letters, 55 (27), 3706-3708 (2014).

“Synthesis of [5-(adenin-9-yl)-2-furyl]methoxymethyl phosphonic acid and evaluations against human adenylate kinases”, M. KACI, J.P. UTTARO, V. LEFORT, C. MATHé, C. EL AMRI, C. Périgaud, Bioorganic & Medicinal Chemistry Letters, 24 (17), 4227-4230 (2014).

“New insight into the mechanism of accumulation and intraerythrocytic compartmentation of albitiazolium, a new type of antimalarial”, S. Wein, C. Tran Van Ba, M. Maynadier, Y. Bordat, J. Perez, S. Peyrottes, L. Fraisse, H. J. Vial, Antimicrobial agents and chemotherapy, 58 (9), 5519-5527 (2014).

“Exploring prodrug approaches for Albitiazolium and its analogues”, S. Peyrottes, S. Caldarelli, S. Wein, C. Périgaud, H. Vial, Current Topics in Medicinal Chemistry, 14 (14), 1653-1667 (2014).

“Synthesis and study of (R)- and (S)- -hydroxyphosphonate acyclonucleosides as structural analogues of (S)-HPMPC (Cidofovir)”, M. KASTHURI, C. El Amri, V. Lefort, C. Périgaud, S. Peyrottes, New Journal of Chemistry, 38 (10), 4736-4742 (2014).

“Synthesis of unnatural 3’-phospha-2’-deoxyfuranose nucleoside analogues”, B. DAYDE, C. PIERRA, G. GOSSELIN, D. SURLERAUX, A.T. ILAGOUMA, J.N. VOLLE, D. VIRIEUX, J.-L. PIRAT, Tetrahedron Letters, 55 (46), 6328-6330 (2014).

“201Tl+-labelled Prussian Blue Nanoparticles as Contrast Agents for SPECT scintigraphy”, M.Perrier, M. Busson, G. Massasso, J. Long, V. Boudousq, J. Pouget, S. PEYROTTES, C. Périgaud, C. Porredon-Guarch, J. de Lapuente, M. Borras, J. Larionova, Y. Guari, Nanoscale, 6 (22), 13425-13429 (2014).

“A Chemical Proteomics Approach for the Search of Pharmacological Targets of the Antimalarial Clinical Candidate Albitiazolium in Plasmodium falciparum Using Photocrosslinking and Click Chemistry”, D.M. PENARETE-VARGAS, A. BOISSON, S. URBACH, H. CHANTELAUZE, S. Peyrottes, L. FRAISSE, H.J. Vial, PLoS ONE, 9 (12), e113918 (2014).

“New carbocyclic nucleoside analogues with a bicyclo[2.2.1]heptane fragment as sugar moiety ; Synthesis, X-ray crystallography and anticancer activity”, CI TĂNASE, C DRĂGHICI, MT CĂPROIU, S SHOVA, C MATHE, FG COCU, C ENACHE, M MAGANU, Bioorganic & Medicinal Chemistry, 22, 513-522 (2014).

“Structure–activity relationships of β-hydroxyphosphonate nucleoside analogues as cytosolic 5′-nucleotidase II potential inhibitors : Synthesis, in vitro evaluation and molecular modeling studies”, M. MEURILLON, Z. MARTON, A. HOSPITAL, L.P. JORDHEIM, J. BEJAUD, C. LIONNE, C. DUMONTET, C. PÉRIGAUD, L. CHALOIN, S. PEYROTTES, European Journal of Medicinal Chemistry, 77, 18-37 (2014).

“Fully validated assay for the quantification of endogenous nucleoside mono- and triphosphates using online extraction coupled with liquid chromatography-tandem mass spectrometry”, C. MACHON, L.P. JORDHEIM, J.-Y. PUY, I. LEFEBVRE, C. DUMONTET, J. GUITTON, Analytical and Bioanalytical Chemistry, 406 (12), 2925-2941 (2014).

“Synthesis of Unnatural Phosphonosugar Analogues”, B. DAYDE, C. PIERRA, G. GOSSELIN, D. SURLERAUX, A.T. ILAGOUMA, C. LABORDE, J.N. VOLLE, D. VIRIEUX, J.-L. PIRAT, European Journal of Organic Chemistry, 2014 (6), 1333-1337 (2014).

“CDP-Ethanolamine and CDP-Choline : One-pot synthesis and 31P NMR study”, S. GHEZAL, M. THOMASSON, I. LEFEBVRE-TOURNIER, C. PERIGAUD, M. A. MACNAUGHTAN, B. ROY , Tetrahedron Letters, 55, 5306-5310 (2014).

Brevet 2014

PCT/FR2014/052447, 29.09.2014.
« Inhibiteurs de 5’-Nucléotidases et leurs utilisations thérapeutiques »
L. Chaloin, S. Peyrottes, C. Lionne, Z. Marton, D. Egron, R. Guillon, C. Périgaud, C. Dumontet, L. Jordheim.


"Synthesis of novel 3’-methyl-5’-norcarbocyclic nucleoside phosphonates as potential anti-HIV agents”, UTTARO J.-P. ; BROUSSOUS S. ; MATHE C. ; PERIGAUD C. ; Tetrahedron, 69, 2131-2136 (2013).

“Identification and characterization of inhibitors of cytoplasmic 5’-nucleotidase cN-II issued from virtual screening”, JORDHEIM L. P ;, MARTON Z. ; RHIMI M ;, CROS-PERRIAL E. ; LIONNE C. ; PEYROTTES S. ; DUMONTET C. ; AGHAJARI N. ; CHALOIN L., Biochemical Pharmacology / Biochemistry and Pharmacology, 85, 497-506 (2013).

“New Bis-thiazolium Analogues as Potential Antimalarial Agents : Design, Synthesis, and Biological Evaluation”, CALDARELLI S. ; EL FANGOUR S. ; WEIN S ;, TRAN VAN BA C. ; PERIGAUD C. ; PELLET A, ; VIAL H. J. ; PEYROTTES S., Journal of Medicinal Chemistry, 56, 496-509 (2013).

“An Alternative Pathway to Ribonucleoside β-Hydroxyphosphonate Analogues and Related Prodrugs”, A.HOSPITAL, M. MEURILLON, S. PEYROTTES, C. PÉRIGAUD, Organic Letters, 15 (18), 4778-4781 (2013).

“Analysis of neutral lipids from microalgae by HPLC-ELSD and APCI-MS/MS”, F. DONOT, G. CAZALS, Z. GUNATA, D. EGRON, J. MALINGE, C. STRUB, A. FONTANA, S. SCHORR-GALINDO, Journal of Chromatography B, 942-943, 98-106 (2013).


“A quantitative liquid chromatography tandem mass spectrometry method for metabolomic analysis of Plasmodium falciparum lipid related metabolites”, VO DUY S ;, BESTEIRO S. ; BERRY L. ; PERIGAUD C. ; BRESSOLLE F. ; VIAL H.J. ; LEFEBVRE-TOURNIER I., Analytica Chimica Acta, 739, 47-55 (2012).

“Choline Analogues in Malaria Chemotherapy”, PEYROTTES S. ; CALDARELLI S. ; WEIN S., PERIGAUD C., PELLET A., VIAL H., Current Pharmaceutical Design, 18, 3454-3466 (2012).

“Synthesis of a new family of acyclic nucleoside phosphonates,analogues of TPases transition states”, DAYDE B. ; BENZARIA S. ; PIERRA C. ; GOSSELIN G. ; SURLERAUX D. ; VOLLE J.-N. ; PIRAT J.-L. ; VIRIEUX D., Organic & Biomolecular Chemistry, 10, 3448-3454 (2012).

“Disulfide Prodrugs of Albitiazolium (T3/SAR97276) : Synthesis and Biological Activities”, CALDARELLI S. ; HAMEL M. ; DUCKERT J.-F. ; OUATTARA M ;. CALAS M.. MAYNADIER M.. SHARON W.. PERIGAUD C.. PELLET A.. VIAL H. J.. PEYROTTES S., Journal of Medicinal Chemistry, 55, 4619-4628 (2012).

“Synthesis of 2’,3’-Dideoxy-2’-fluoro-3’-(hydroxyimino)-, -3’-(methoxyimino)- and -3’-(hydroxyamino)pyrimidine Nucleosides”, KHALIL A. ; MATHE C. ; PERIGAUD C., European Journal of Organic Chemistry, 3172-3179 (2012).


“Structural Insights into the Inhibition of Cytosolic 5’-Nucleotidase II (cN-II) by Ribonucleoside 5’-Monophosphate Analogues ”,
GALLIER F. ; LALLEMAND P. ; MEURILLON M ;, JORDHEIM L, ; DUMONTET C. ; PERIGAUD C. ; LIONNE C. ; PEYROTTES S, ; CHALOIN L., PLoS Computational Biology, 7, e1002295 (2011).

“Synthetic Studies towards New Nucleoside Analogues : Preparation of (±)-1’,4’-Dimethyladenosine”, CHAUBET, G. ; BOURGEOIS, D. ; PÉRIGAUD, C., European Journal of Organic Chemistry, (2), 319-326 (2011).

“Synthesis of 2′,3′-Dideoxynucleoside Phosphoesters Using H-Phosphonate Chemistry on Soluble Polymer Support.” CRAUSTE, C. ; PÉRIGAUD, C. ; PEYROTTES, S., Journal of Organic Chemistry, 76 (3), 997-1000 (2011).

“A facile and effective synthesis of lamivudine 5’-diphosphate.” ROY, B. ; LEFEBVRE, I. ; PUY, J.-Y. ; PÉRIGAUD, C., Tetrahedron Letters, 52, 1250-1252 (2011).

“Synthesis of (R)- and (S)-ßhydroxyphosphonate acyclonucleosides : structural analogues of Adefovir (PMEA) .” KASTHURI M. ; CHALOIN L. ; PERIGAUD C. ; PEYROTTES S., Tetrahedron Asymmetry, 22, 1505-1511 (2011).

“5 ’,6 ’-Nucleoside Phosphonate Analogues Architecture : Synthesis and Comparative Evaluation towards Metabolic Enzymes.” GALLIER, F. ; ALEXANDRE, J. A. C. ; EL AMRI, C. ; DEVILLE-BONNE, D. ; PEYROTTES, S. ; PERIGAUD, C., ChemMedChem, 6, 1094-1106 (2011).

“Synthesis of Pyrimidine-Containing Nucleoside β-(R/S)-Hydroxyphosphonate Analogues.” MEURILLON, M. ; CHALOIN, L. ; PÉRIGAUD, C. ; PEYROTTES, S. ; PERIGAUD, C., European Journal of Organic Chemistry, (20-21), 3794-3802 (2011).

“Interaction of Human 3-Phosphoglycerate Kinase with Its Two Substrates : Is Substrate Antagonism a Kinetic Advantage ? ” LALLEMAND, P. ; CHALOIN, L. ; ROY, B. ; BARMAN, T. ; BOWLER, M. W. ; LIONNE, C., Journal of Molecular Biology, 409 (5), 742-757 (2011).


“Diastereoselective synthesis of (±)-1’,4’-dimethyluridine”, SAUTREY, G. ; BOURGEOIS, D. ; PÉRIGAUD, C., Organic and Biomolecular Chemistry, 8, (22), 378-383 (2010).

“Exploring metabolomic approaches to analyse phospholipids biosynthetic pathways in Plasmodium”, BESTEIRO, S. ; VO DUY, S. ; PÉRIGAUD, C. ; TOURNIER, I. ; VIAL, H.J., Parasitology, 137, (SI 9), 1343-1356 (2010).

“Diels–Alder reaction of vinylene carbonate and 2,5-dimethylfuran : kinetic vs. thermodynamic control” TAFFIN, C. ; KREUTLER, G. ; BOURGEOIS, D. ; CLOT, E. ; PÉRIGAUD, C., New Journal of Chemistry, 34, 517-525 (2010).

“Rationally designed aptamer-based fluorescence polarization sensor dedicated to the small target analysis.” PERRIER, S. ; RAVELET, C. ; GUIEU, V. ; FIZE, J. ; ROY, B. ; PÉRIGAUD, C. ; PEYRIN, E., Biosensors & Bioelectronics, 25, (7), 1652-1657 (2010).

“Reliability of Antimalarial Sensitivity Tests Depends on Drug Mechanisms of Action.” WEIN, S. ; MAYNADIER, M. ; VAN BA, C. T. ; CERDAN, R. ; PEYROTTES, S. ; FRAISSE, L. ; VIAL, H., Journal of Clinical Microbiology, 48 (5), 1651-1660 (2010).

“F1-Adenosine Triphosphatase Displays Properties Characteristic of an Antigen Presentation Molecule for Vgamma9Vdelta2 T Cells.” MOOKERJEE-BASU, J. ; VANTOUROUT, P. ; MARTINEZ, L. O. ; PERRET, B. ; COLLET, X. ; PÉRIGAUD, C. ; PEYROTTES, S. ; CHAMPAGNE, E., Journal of Immunology, 184 (12), 6920-6928 (2010).

“Exploration of potential prodrug approach of the bis-thiazolium salts T3 and T4 for orally delivered antimalarials.” CALDARELLI, S. A. ; BOISBRUN, M. ; ALARCON, K. ; HAMZE, A. ; OUATTARA, M. ; SALOM-ROIG, X. ; MAYNADIER, M. ; WEIN, S. ; PEYROTTES, S. ; PELLET, A. ; CALAS, M. ; VIAL, H., Bioorganic & Medicinal Chemistry Letters, 20 (13), 3953-3956 (2010).

“Multiplexed Detection of Small Analytes by Structure-Switching Aptamer-Based Capillary Electrophoresis.” ZHU, Z. Y. ; RAVELET, C. ; PERRIER, S. ; GUIEU, V. ; ROY, B. ; PÉRIGAUD, C. ; PEYRIN, E., Analytical Chemistry, 82 (11), 4613-4620 (2010).

“Synthesis and evaluation of new bis-thiazolium salts as potential antimalarial drugs.” CALDARELLI, S. ; DUCKERT, J.-F. ; WEIN, S. ; CALAS, M. ; PÉRIGAUD, C. ; VIAL, H. ; PEYROTTES, S., Chemmedchem, 5 (7), 1102-1109 (2010).

“Rapid synthesis of 2’,3’-dideoxy-3’[beta]-fluoro-pyrimidine nucleosides from 2’-deoxypyrimidine nucleosides.” KHALIL, A. ; MATHÉ, C. ; PÉRIGAUD, C., Bioorganic Chemistry, 38 (6), 271-274 (2010).

“Synthesis of the natural enantiomer of neplanocin B.” HAMON, N. ; UTTARO, J.-P. ; MATHÉ, C. ; PÉRIGAUD, C., Bioorganic Chemistry, 38 (6), 275-278 (2010).


« Inclusion complexes of a nucleotide analogue with hydroxypropyl-beta-cyclodextrin », JORDHEIM L.P., DEGOBERT G., DIAB R., PEYROTTES S., PÉRIGAUD C., DUMONTET C. & FESSI H., J Incl Phenom Macrocycl Chem, 63 (1-2), 11-16 (2009).

« Aptamer-Modified Micellar Electrokinetic Chromatography for the Enantioseparation of Nucleotides », RUTA J., PERRIER S., RAVELET C., ROY B., PERIGAUD C. & PEYRIN E., Analytical Chemistry, 81 (3), 1169-1176 (2009).doi:10.1021/ac802443j

« Molecularly imprinted polymer for analysis of zidovudine and stavudine in human serum by liquid chromatography-mass spectrometry », VO DUY S., LEFEBVRE-TOURNIER I., PICHON V., HUGON-CHAPUIS F., PUY J.-Y. & PERIGAUD C., Journal of Chromatography B, 877 (11-12), 1101-1108 (2009).

“Development of a sensitive and selective LC/MS/MS method for the simultaneous determination of intracellular araCTP, CTP and dCTP in human follicular lymphoma cell line”, CRAUSTE C., LEFEBVRE I., HOVANESSIAN M., PUY J.Y., ROY B., PEYROTTES S., GUITTON J., DUMONTET C. & PERIGAUD C., Journal of Chromatography B, 877 (14-15), 1417-1425 (2009).doi:10.1016/j.jchromb.2009.02.071

“Developing an efficient route to the synthesis of nucleoside 1-alkynykphosphonates.” MEURILLON, M. ; GALLIER, F. ; PEYROTTES, S. ; PÉRIGAUD, C., Tetrahedron, 65, (31), 6039-604 (2009).

“Special feature of mixed phosphotriester derivatives of cytarabine.” GOUY, M.-H. ; JORDHEIM, L. P. ; LEFEBVRE, I. ; CROS, E. ; DUMONTET, C. ; PEYROTTES, S. ; PÉRIGAUD, C., Bioorganic & Medicinal Chemistry, 17, (17), 6340-6347 (2009).

“Specific Requirements for Vgamma9Vdelta2 T Cell Stimulation by a Natural Adenylated Phosphoantigen.” VANTOUROUT, P. ; MOOKERJEE-BASU, J. ; ROLLAND, C. ; PONT, F. ; MARTIN, H. ; DAVRINCHE, C. ; MARTINEZ, L. O. ; PERRET, B. ; COLLET, X. ; PERIGAUD, C. ; PEYROTTES, S. ; CHAMPAGNE, E., Journal of Immunology, 183, (6), 3848-3857 (2009).

“Separation of diastereoisomers of Ara-C phosphotriesters using solid phase extraction and HPLC for the study of their decomposition kinetic in cell extracts.” FOULON, C. ; TEDOU, S. ; PEYROTTES, S. ; PÉRIGAUD, C. ; BONTE, J.P. ; VACCHER, C. ; GOOSENS, J.F., Journal of Chromatography B, 877, (29), 3475-3481 (2009).

“Simultaneous analysis of eight nucleoside triphosphates in cell lines by liquid chromatography coupled with tandem mass spectrometry.” COHEN, S. ; MEGHERBI, M. ; JORDHEIM, L.P. ; LEFEBVRE, I. ; PÉRIGAUD, C. ; DUMONTET, C. ; GUITTON, J., Journal of Chromatography B, 877, (30), 3831-3840 (2009).

“Decomposition of AZTMP prodrugs in biological media studied by on-line solid-phase extraction coupled to liquid chromatography mass spectrometry”, LEFEBVRE I., BELTRAN T., PEYROTTES S. & PERIGAUD C., Biomedical Chromatography, 23, (11), 1160-1168 (2009).

“Insights into the Soluble PEG-Supported Synthesis of Cytosine-Containing Nucleoside 5’-Mono-, Di-, and Triphosphates.” CRAUSTE, C. L. ; PÉRIGAUD, C. ; PEYROTTES, S., Journal of Organic Chemistry, 74, (23), 9165-9172 (2009).


« Recent approaches in the synthesis of conformationally restricted nucleoside analogues », C. MATHE & C. PÉRIGAUD, European Journal of Organic Chemistry, 1489-1905 (2008). doi : 10.1002/ejoc.200700946

« Interaction of human 3-phosphoglycerate kinase with L-ADP, the mirror image of D-ADP ».A. VARGA, J. SZABÓ, B. FLACHNER, B. ROY, P. KONAREV, D. SVERGUN, P. ZÁVODSZKY, C. PÉRIGAUD, T. BARMAN, C. LIONNE and M. VAS, Biochemical and Biophysical Research Communications, 366 (4), 994-1000. (2008). doi:10.1016/j.bbrc.2007.12.061

« Molecular basis for the lack of enantioselectivity of human 3-phosphoglycerate kinase », GONDEAU C., CHALOIN L., LALLEMAND P., ROY B., PÉRIGAUD C., BARMAN T., VARGA A., VAS M., LIONNE C., & AROLD S.T., Nucleic Acids Research, 36 (11), 3620-3629 (2008). doi:10.1093/nar/gkn212

« Differences in the transient kinetics of the binding of D-ADP and its mirror image L-ADP to human 3-phosphoglycerate kinase revealed by the presence of 3-phosphoglycerate », GONDEAU C., CHALOIN L., VARGA A., ROY B., LALLEMAND P., PÉRIGAUD C., BARMAN T., VAS M., & LIONNE C., Biochemistry, 47 (11), 3462-3473 (2008).

« Phenyl phosphotriester derivatives of AZT : Variations upon the SATE moiety », VILLARD A.-L., COUSSOT G., LEFEBVRE I., AUGUSTIJNS P., AUBERTIN A.-M., GOSSELIN G., PEYROTTES S. & PÉRIGAUD C., Bioorganic & Medicinal Chemistry, 16 (15), 7321-7329 (2008).

« Synthesis of 3’-deoxy-3’-C-methyl nucleoside derivatives », ALJARAH M., COUTURIER S., MATHE C. & PÉRIGAUD C., Bioorganic & Medicinal Chemistry, 16 (15), 7436-7442 (2008).

« Separation of nucleoside phosphoramidate diastereoisomers by high performance liquid chromatography and capillary electrophoresis »,
GOOSSENS J.F., ROUX S., EGRON D., PÉRIGAUD C., BONTE J.P., VACCHER C. and FOULON C., Journal of Chromatography B, 875 (1), 288-295 (2008)

« Electrospray ionization mass spectrum of S-Acyl-2-thioethyl phosphoramidate diester derivatives », JIN P., JI S.H., EGRON D. & PERIGAUD C., International Journal of Mass Spectrometry, 274, 70-74 (2008)


« Ex-chiral-pool synthesis of beta-hydroxyphosphonate nucleoside analogues », F. GALLIER, S. PEYROTTES & C. PÉRIGAUD, European Journal of Organic Chemistry, (6), 925-933 (2007). doiI:10.1002/ejoc.200600562

« Enantioselectivity of human AMP, dTMP and UMP-CMP kinases », J. A. C. ALEXANDRE, B. ROY, D. TOPALIS, S. POCHET, C. PÉRIGAUD & D. DEVILLE-BONNE, Nucleic Acids Research, 35 (14), 4895-4904 (2007). doi:10.1093/nar/gkm479

« First enantioselective synthesis of (−)-neplanocin F », S. RODRIGUEZ, D. EDMONT,, C. MATHÉ & C. PÉRIGAUD, Tetrahedron, 63 (30), 7165-7171 (2007). doi:10.1016/j.tet.2007.04.094

« Synthesis of 3’-deoxy-3’-C-methyl-beta-D-ribonucleoside analogs », S. COUTURIER, M. ALJARAH, G. GOSSELIN, C. MATHE & C. PERIGAUD, Tetrahedron, 63 (46), 11260-11266 (2007).doi:10.1016/j.tet.2007.08.092

“Probing of PSE acetal protection for nucleoside chemistry« J. P. UTTARO, L. UTTARO, A. TATIBOUET, P. ROLLIN, C. MATHÉ & C. PÉRIGAUD, Tetrahedron Letters, 48 (22), 3851-3854 (2007).doi:10.1016/j.tetlet.2007.03.153 »Quantification of zidovudine and its monophosphate in cell extracts by on-line solid-phase extraction coupled to liquid chromatography", I. LEFEBVRE, J.-Y. PUY, C. PERRIN & C. PÉRIGAUD, Journal of Chromatography B, , 858 (1-2), 2-7 (2007). doi:10.1016/j.jchromb.2007.07.028


« Quantification of 5 ’-monophosphate cytosine arabinoside (Ara-CMP) in cell extracts using liquid chromatography-electrospray mass spectrometry », M.-H. GOUY, H. FABRE, M.-D. BLANCHIN, S. PEYROTTES, C. PERIGAUD & I. LEFEBVRE, Analytica Chimica Acta, 566 (2), 178-184 (2006). doi:10.1016/j.aca.2006.02.058

“L-Nucleoside enantiomers as antiviral drugs : a mini-review”, C. MATHÉ & G. GOSSELIN, Antiviral Research, 71, 276-281 (2006). doi:10.1016/j.antiviral.2006.04.017

“Synthesis and conformational analysis of C-4’ modified (2-oxabicyclo[3.1.0]hexyl) pyrimidine nucleosides”, J. GAGNERON, G. GOSSELIN & C. MATHÉ, European Journal of Organic Chemistry, 4891-4897 (2006). doi : 10.1002/ejoc.200600550

« Separation of 3 ’-azido-2 ’,3 ’-dideoxythymidine pronucleotide diastereoisomers in biological samples by CZE with cyclodextrin addition », C. PERRIN, G. COUSSOT, I. LEFEBVRE, C. PÉRIGAUD & H. FABRE, Journal of Chromatography A, 1111 (2), 139-146 (2006).doi:10.1016/j.chroma.2005.05.099

“Structure activity relationship of uridine 5’-diphosphate analogues at the human P2Y6 receptor”, P. BESADA, D. H. SHIN, S. COSTANZI, H. KO, C. MATHÉ, J. GAGNERON, G. GOSSELIN, S. MADDILETI, T. K. HARDEN & K. A. JACOBSON, Journal of Medicinal Chemistry, 49, 5532-5543 (2006). DOI : 10.1021/jm060485n

“Diastereoisomeric resolution of a pronucleotide using solid phase extraction and high performance liquid chromatography : Application to a stereoselective decomposition kinetic in cell extracts« , C. FOULON, C. VACCHER, A.-L. VILLARD, J.-Y. PUY, I. LEFEBVRE, C. PÉRIGAUD, J.-P. BONTE & J.-F. GOOSSENS, Journal of Pharmaceutical & Biomedical Analysis, 42 (2), 245-252 (2006).doi:10.1016/j.jpba.2006.04.033 »Use of microwave irradiation for sugar and nucleoside phosphonates synthesis", S. PEYROTTES, F. GALLIER, J. BEJAUD & C. PÉRIGAUD, Tetrahedron Letters, 47 (44), 7719-7721 (2006).doi:10.1016/j.tetlet.2006.08.116



Perigaud, Christian ; Peyrottes, Suzanne ; Dumontet, Charles. Preparation of phosphoester prodrugs of gemcitabine as anticancer agents. PCT Int. Appl. (2009), 32pp. WO 2009053654

Peyrottes, Suzanne ; Perigaud, Christian ; Crauste, Céline, « Method for preparing nucleotides and related analogues by synthesis on soluble substrate, and biological tools thus prepared », WO 2009/115694, 24.09.2009.


Sommadossi, Jean-Pierre ; Gosselin, Gilles ; Pierra, Claire ; Perigaud, Christian ; Peyrottes, Suzanne. Compounds and Pharmaceuticals compositions for the treatment of viral infections. PCT Int. Appl. (2008), 273pp. CODEN : PIXXD2 WO 2008082601 A2

Sommadossi, Jean-Pierre ; Gosselin, Gilles ; Pierra, Claire ; Perigaud, Christian ; Peyrottes, Suzanne. Compounds and Pharmaceuticals compositions for the treatment of liver disorders. PCT Int. Appl. (2008), 109pp. CODEN : PIXXD2 WO 2008082602


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