E5 – Publications

E5 – Publications 2019-06-04T15:22:17+00:00


Synthèse organique

  1. Castelli U., Lohier J.-F., Drukenmüller I., Mingot A., Bachman C., Alayrac C., Marrot J., Stierstorfer K., Kornath A., Gaumont A.-C., Thibaudeau S., Evidence of Phosphonium-Carbenium Dication Formation in a Superacid: Precursor to Fluorinated Phosphine Oxides, Angew. Chem. Int. Ed. (2019) 58, 1355-1360. DOI:10.1002/anie.201811032.

  2. Auberger N., Onfroy B., Fontelle, N., Foucart Q., Blériot Y., Lewis acid-catalysed nucleophilic opening of a bicyclic hemiaminal followed by ring contraction: Access to functionalized L-idonojirimycin derivatives, Carbohydrate Res. (2019) 472, 65-71. DOI:10.1016/j.carres.2018.11.008.

  3. Uehara A., Olivero S., Michelet B., Martin-Mingot A., Thibaudeau S., Duñach E., Direct and Selective C-H Carbamoylation of (Hetero)aromatics with TMSOTf-Activated Carbamoyl Chloride, Eur. J. Org. Chem. (2019) 46-49. DOI:10.1002/ejoc.201801338 (Very Important Paper).

  4. Caillaud M., Guillard J., Richard D., Milin S., Chassaing D., Paccalin M., Page G., Rioux Bilan A., Trans ε viniferin decreases amyloid deposits and inflammation in a mouse transgenic Alzheimer model, PLoS ONE (2019) 14, e021266. DOI:10.1371/journal.pone.02121663.

  5. Viricel W., Fournet G., Beaumel S., Perrial E., Papot S., Dumontet C., Joseph B., Monodisperse polysarcosine-based highly-loaded antibody-drug conjugates, Chem. Sci. (2019) 10, 4048-4053. DOI:10.1039/c9sc00285e.

  6. Porte K., Renoux B., Péraudeau E., Clarhaut J., Eddhif B., Poinot P., Gravel E., Doris E., Wijkhuisen A., Audisio D., Papot S., Taran F., Controlled Release of a Micelle Payload via Sequential Enzymatic and Bioorthogonal Reactions in Living Systems, Angew. Chem. Int. Ed. (2019) 58, 6366-6370. DOI:10.1002/anie.201902137.

  7. Chany A.-C., Legros F., Haroun H., Kundu U. K., Biletskyi B., Torlak S., Mathé-Allainmat M., Lebreton J., Macé A., Carboni B., Renoux B., Gosselin P., Dujardin G., Gaulon-Nourry C., Function-Oriented Synthesis toward Peloruside A Analogues, Org. Lett. (2019) 21, 2988-2992. DOI:10.1021/acs.orglett.9b00413 (front cover).

  8. Zhu S., Tran A. T., Hirokami Y., Gontard G., Khaled O., Zhang Y., Kato A., Blériot Y., Sollogoub M., Bi(OTf)3-mediated intramolecular epoxide opening for bicyclic azepane synthesis, J. Carb. Chem. (2019) 38, 139-149. DOI:10.1080/07328303.2019.1581887.

  9. Hansen T., Lebedel L., Remmerswaal W. A., van der Vorm S., Wander D. P. A., Somers M., Overkleeft H. S., Filippov D. V., Désiré J., Mingot A., Blériot Y., van der Marel G. A., Thibaudeau S., Codée J. D. C., Defining the SN1 side of glycosylation reactions: stereoselectivity of glycopyranosyl cations, ACS Cent. Sci. (2019) 5, 781-788. DOI:10.1021/acscentsci.9b00042 (front cover).

  10. Thomas M., Alsarraf J., Araji N., Tranoy-Opalinski I., Renoux B., Papot S., The Lossen rearrangement from free hydroxamic acids, Org. Biomol. Chem. (2019) Advance Article. DOI:10.1039/c9ob00789j.

  11. Foucart Q., Marrot J., Désiré J., Blériot Y., Site-Selective Debenzylation of C-Allyl Iminosugars Enables Their Stereocontroled Structure Diversification at the C-2 Position, Org. Lett. (2019) Article ASAP. DOI:10.1021/acs.orglett.9b01712.

  1. Eddhif B., Lange J., Guignard N., Batonneau Y., Clarhaut J., Papot S., Geffroy-Rodier C., Poinot P., Study of a novel agent for TCA precipitated proteins washing – comprehensive insights into the role of ethanol/HCl on molten globule state by multi-spectroscopic analyses, J. Prot. (2018) 173, 77-88. DOI:10.1016/j.jprot.2017.11.016.

  2. Péraudeau E., Cronier L., Monvoisin A., Poinot P., Mergault C., Guilhot F., Tranoy-Opalinski I., Renoux B., Papot S., Clarhaut J., Enhancing tumor response to targeted chemotherapy through up-regulation of folate receptor α expression induced by dexamethasone and valproic acid, J. Cont. Rel. (2018) 269, 36-44. DOI:10.1016/j.jconrel.2017.11.011.

  3. Eddhif B., Guignard N., Batonneau Y., Clarhaut J., Papot S., Geffroy-Rodier C., Poinot P., TCA precipitation and ethanol/HCl single-step purification evaluation: One-dimensional gel electrophoresis, bradford assays, spectrofluorometry and Raman spectroscopy data on HSA, Rnase, lysozyme – Mascots and Skyline data, Data in Brief (2018) 17, 938-953. DOI:10.1016/j.dib.2018.01.095.

  4. Koniev O., Dovgan I., Renoux B., Ehkirch A., Eberova J., Cianférani S., Kolodych S., Papot S., Wagner A., Reduction–rebridging strategy for the preparation of ADPN-based antibody–drug conjugates, Med. Chem. Commun. (2018) 9, 827-830. DOI:10.1039/c8md00141c.

  5. Métayer B., Angeli A., Mingot A., Jouvin K., Evano G., Supuran C.T., Thibaudeau S., Fluoroenesulphonamides: N-sulphonylurea isosteres showing nanomolar selective cancer-related transmembrane human carbonic anhydrase inhibition, J. Enz. Inhib. Med. Chem. (2018) 33, 804-808. DOI:10.1080/14756366.2018.1461097.

  6. Michelet B., Carreyre H., Lecornué F., Mingot A., Thibaudeau S., Superelectrophilic activation in superacid HF/SbF5: Expanding molecular diversity in nitrogen-containing compounds series by fluorination, J. Fluor. Chem. (2018) 214, 68-79. DOI:10.1016/j.jfluchem.2018.04.017.

  7. Fontelle N., Yamamoto A., Arda A., Jiménez-Barbero J., Kato A., Désiré J., Blériot Y., 2-Acetamido-2-deoxy-L-iminosugar C-alkyl and C-aryl glycosides: synthesis and glycosidase inhibition, Eur. J. Org. Chem. (2018) 40, 5477-5488. DOI:10.1002/ejoc.201800678.

  8. Amaniampong N., Clément J.-L., Gigmes D., Ortiz Mellet C., García Fernández J. M., Blériot Y., Chatel G., De Oliveira Vigier K., Jérôme F., Catalyst-free synthesis of alkylpolyglycosides induced by high frequency ultrasound, ChemSusChem (2018) 11, 2673-2676. DOI:10.1002/cssc.201801137.

  9. Compain G., Oumata N., Clarhaut J., Péraudeau E., Renoux B., Galons H., Papot S., A β-glucuronidase-responsive albumin-binding prodrug for potential selective kinase inhibitor-based cancer chemotherapy, Eur. J. Med. Chem. (2018) 158, 1-6. DOI:10.1016/j.ejmech.2018.08.100.

  10. Renoux B., Fangous L., Hötten C., Péraudeau E., Eddhif B., Poinot P., Clarhaut J., Papot S., A β-glucuronidase-responsive albumin-binding prodrug programmed for the double release of monomethylauristatin E, MedChemComm (2018) 9, 2068-2071. DOI:10.1039/C8MD00466H.

  1. Tawk A., Deborde M., Labanowski J., Thibaudeau S., Gallard H., Transformation of the Β-Triketone Pesticides Tembotrione and Sulcotrione by Reactions with Ozone: Kinetic Study, Transformation Products, Toxicity and Biodegradability, Ozone: Science & Engineering (2017) 39, 3-13. DOI: 10.1080/01919512.2016.1257933.

  2. Bonazaba Milandou L. J. C., Carreyre H., Alazet S., Greco G., Martin-Mingot A., Nkounkou Loumpangou C., Ouamba J.-M., Bouazza F., Billard T., Thibaudeau S., Superacid-Catalyzed Trifluoromethylthiolation of Aromatic Amines, Angew. Chem. Int. Ed. (2017) 56, 169-172. DOI: 10.1002/anie.201609574.

  3. Probst N., Martin A., Désiré J., Mingot A., Marrot J., Blériot Y., Thibaudeau S., HF-Induced Intramolecular C‑Arylation and C‑Alkylation/Fluorination of 2‑Aminoglycopyranoses, Org. Lett. (2017) 19, 1040-1043. DOI: 10.1021/acs.orglett.7b00003.

  4. Renoux B., Raes F., Legigan T., Péraudeau E., Eddhif B., Poinot P., Tranoy-Opalinski I., Alsarraf J., Koniev O., Kolodych S., Lerondel S., Le Pape A., Clarhaut J., Papot S., Targeting the tumour microenvironment with an enzyme-responsive drug delivery system for the efficient therapy of breast and pancreatic cancers, Chem. Sci. (2017) 8, 3427-3433. DOI: 10.1039/c7sc00472a.

  5. Vadlamani G., Stubbs K. A., Désiré J., Blériot Y., Vocadlo D. J., Mark B. L., Conformational flexibility of the glycosidase NagZ allows it to bind structurally diverse inhibitors to suppress β-lactam antibiotic resistance, Protein Science (2017) 26, 1161-1170. DOI: 10.1002/pro.3166.

  6. Bezagu M., Clarhaut J., Renoux B., Monti F., Tanter M., Tabeling P., Cossy J., Couture O., Papot S., Arseniyadis S., In situ targeted activation of an anticancer agent using ultrasound-triggered release of composite droplets, Eur. J. Med. Chem. (2017) 142, 2-7 DOI: 10.1016/j.ejmech.2017.03.057.

  7. Theunissen C., Métayer B., Lecomte M., Henry N., Chan H.-C., Compain G., Gérard P., Bachmann C., Mokhtari N., Marrot J., Martin-Mingot A., Thibaudeau S., Evano G., Cationic polycyclization of ynamides: building up molecular complexity, Org. Biomol. Chem. (2017) 15, 4399-4416. DOI: 10.1039/c7ob00850c.

  8. Bouquet J., King D. T., Vadlamani G., Benzie G. R., Iorga B., Ide D., Adachi I., Kato A., Vocadlo D. J., Mark B. L., Blériot Y., Désiré J., Selective trihydroxylated azepane inhibitors of NagZ, a glycosidase involved in Pseudomonas aeruginosa resistance to β-lactam antibiotics, Org. Biomol. Chem. (2017) 15, 4609-4619. DOI: 10.1039/c7ob00838d.

  9. Carreyre H., Carré G., Ouedraogo M., Vandebrouck C., Bescond J., Supuran C. T., Thibaudeau S., Bioactive Natural Product and Superacid Chemistry for Lea Compound Identification: A Case Study of Selective hCA III and L-Type Ca2+ Current Inhibitors for Hypotensive Agent Discovery, Molecules (2017) 22, 915. DOI: 10.3390/molecules22060915.

  10. Alvarez-Dorta D., King D. T., Legigan T., Ide D., Adachi I., Deniaud D., Désiré J., Kato A., Vocadlo D., Gouin S. G., Blériot Y., Multivalency to inhibit and discriminate hexosaminidases, Chem. Eur. J. (2017) 23, 9022-9025. DOI: 10.1002/chem.201701756.

  11. Tamigney Kenfack M., Mazur M., Nualnoi T., Shaffer T. L., Ngassimou A., Blériot Y., Marrot, J., Marchetti R., Sintiprungrat K., Chantratita N., Silipo A., Molinaro A., AuCoin D. P., Burtnick M. N., Brett P. J., Gauthier C., Deciphering minimal antigenic epitopes associated with Burkholderia pseudomallei and Burkholderia mallei lipopolysaccharide O-antigens, Nat. Comm. (2017) 8, 115. DOI: 10.1038/s41467-017-00173-8.

  12. Kolodych S., Michel C., Delacroix S., Koniev O., Ehkirch A., Eberova J., Cianférani S., Renoux B., Krezel W., Poinot P., Muller C. D., Papot S., Wagner A., Development and evaluation of β-galactosidase-sensitive antibody-drug conjugates, Eur. J. Med. Chem. (2017) 142, 376-382. DOI: 10.1016/j.ejmech.2017.08.008.

  13. Kato A., Nakagome I., Nakawaga S., Kinami K., Adachi I., Jenkinson S. F., Désiré J., Blériot Y., Nash R. J., Fleet G. W. J., Hirono S., In silico analyses of essential interactions of iminosugars with the HexA active site and evaluation of their pharmacological chaperone effects for Tay-Sachs disease, Org. Biomol. Chem. (2017) 15, 9297-9304. DOI: 10.1039/c7ob02281f.


    1. Lavoie S., Ouellet M., Fleury P.-Y., Gauthier C., Legault J., Pichette A., Complete 1H and 13C NMR assignments of a series of pergalloylated tannins, Magn. Reson. Chem. (2016) 54, 168-174.

    1. Zwick V., Nurisso A., Simoes-Pires C., Bouchet S., Martinet N., Lehotzky A., Ovadi J., Cuendet M., Blanquart C., Bertrand P., Cross metathesis with hydroxamate and benzamide BOC-protected alkenes to access HDAC inhibitors and their biological evaluation highlighted intrinsic activity of BOC-protected dihydroxamates, Bioorg. Med. Chem. Lett. (2016) 26, 154-159.
    1. A. Le Darz, U. Castelli, N. Mokhtari, A. Martin-Mingot, J. Marrot, F. Bouazza, O. Karam, S. Thibaudeau, Tandem superelectrophilic activation for the regioselective chlorofluorination of recalcitrant allylic amines, Tetrahedron (2016) 72, 674-689.
    1. Martin A., Arda A., Désiré J., Martin-Mingot A., Probst N., Sinaÿ P., Jiménez-Barbero J., Thibaudeau S., Blériot Y., Catching elusive glycosyl cations in a condensed phase with HF/SbF5 superacid, Nature Chemistry (2016) 8, 186-191.
    1. El Bahhaj F., Denis I., Pichavant L., Delatouche R., Collette F., Linot C., Pouliquen D., Grégoire M., Héroguez V., Blanquart C., Bertrand P., Histone Deacetylase Inhibitors Delivery using Nanoparticles with Intrinsic Passive Tumor Targeting Properties for Tumor Therapy, Theranostic (2016), 6, 795-807.
    1. G. Evano, N. Blanchard, G. Compain, A. Coste, C.S. Demmer, W. Gati, C. Guissar, J. Heimburger, N. Henry, K. Jouvin, G. Karthikeyan, A. Laouiti, M. Lecomte, A. Martin-Mingot, B. Métayer, B. Michelet, A.E. Nitelet, C. Theunissen, S. Thibaudeau, J. Wang, M. Zarca, C. Zhang, A Journey in the Chemistry of Ynamides: from Synthesis to Applications, Chemistry Letters, 2016, 45, (6), 574-585.
    1. J. Roche, P. Bertrand. Inside HDAC with more selective HDAC inhibitors. Eur. J. Med. Chem. (2016), online.
  1. Pairault N., Barat R., Tranoy-Opalinski I., Renoux B., Thomas M., Papot S., Rotaxane-based architecture for biological applications, C. R Chimie (2016), 19, 103-112.
  2. Rubio S., Clarhaut J., Péraudeau E., Vincenzi M., Soum C., Rossi F., Guillon J., Papot S., Ronga L., Diminished oligomerization in the synthesis of new anti-angiogenic cyclic peptide using solution instead of solid-phase cyclization, Biopolymers (2016), 368-375.

  3. Mazur M., Barycza B., Andriamboavonjy H., Lavoie S., Tamigney Kenfack M., Laroussarie A., Blériot Y., Gauthier C., 4′-Methoxyphenacyl-Assisted Synthesis of β‑Kdo Glycosides, J. Org. Chem. (2016) 81, 10585-10599. DOI: 10.1021/acs.joc.6b01431

  4. Zimmermann L., Das I., Désiré J., Sautrey G., Barros V., El Khoury M., Mingeot-Leclercq M.-P., Décourt J.-L., New Broad-Spectrum Antibacterial Amphiphilic Aminoglycosides Active against Resistant Bacteria: From Neamine Derivatives to Smaller Neosamine Analogues, J. Med. Chem. (2016) 59, 9350-9369. DOI: 10.1021/acs.jmedchem.6b00818


    1. Aloui L., Zouari S., Kossentini M., Geffroy C., Guillard J., Phytochemical Investigation, Isolation and Characterization of Coumarins from Aerial Parts and Roots of Tunisian Pituranthos Chloranthus (Apiaceae), Pharmacognosy Communications (2015) 5, 237-243.
    1. Barat R., Legigan T., Tranoy-Opalinski I., Renoux B., Peraudeau E., Clarhaut J., Poinot P., Fernandes A. E., Aucagne V., Leigh D. A. and Papot S., A mechanically interlocked molecular system programmed for the delivery of an anticancer drug, Chem Sci. (2015) 6, 2608-2613.
    1. Bensalma S., Chadeneau C., Legigan T., Renoux B., Gaillard A., De Boisvillers S., Pinet-Charvet S., Papot S., Muller J-M., Evaluation of cytotoxic properties of a cyclopamine glucuronide prodrug in rat glioblastoma cells and tumors, J. Mol. Neurosci.(2015) 55, 51-61.
    1. Bouclé S., Melin C., Clastre M., Guillard J., Design, synthesis and Evaluation of new marine alkaloid-derived pentacyclic structures with anti-tumoral potency, Mar. Drugs, (2015) 13, 655-665.
    1. Carre G., Ouedraogo M., Magaud C., Carreyre H., Becq F., Bois P., Supuran C. T., Thibaudeau S., Vandebrouck C., Bescond J., Vasorelaxation induced by dodoneine is mediated by calcium channels blockade and carbonic anhydrase inhibition on vascular smooth muscle cells, J. Ethnopharmacology (2015) 169, 8-17.
    1. Gharbi A., Legigan T., Humblot V., Papot S., Berjault J.-M., Surface functionalization by covalent immobilization of an innovative carvacrol derivative to avoid fungal biofilm formation, ABM Express (2015), 5:9.
    1. Jagadeesh Y., Tuan A. T., Luo B., Auberger N., Désiré J., Nakagawa S., Kato A., Zhang Y., Sollogoub M., Blériot Y., g-Aminoalcohol rearrangement applied to pentahydroxylated azepanes provides pyrrolidines epimeric to homoDMDP, Org. Biomol. Chem. (2015) 13, 3446-3456.
    1. Lavoie S., Gauthier C., Mshvildadze V., Legault J., Roger B., Pichette A., DFT calculations and ROESY NMR data for the diastereochemical characterization of cytotoxic tetraterpenoids from the oleoresin of Abies balsamea, J. Nat. Prod. (2015) 78, 2896-2907.
    1. Le Darz A., Mingot A., Bouazza F., Castelli U., Karam O., Tanc M., Supuran C. T., Thibaudeau S., Fluorinated pyrolidines and piperidines incorporating tertiary benzenesulfonamide moieties are selective carbonic anhydrase II inhibitors, J. Enz. Inhib. Med. Chem. (2015) 30, 737-745.
    1. Marchetti R., Dillon M. J., Burtnick M. N., Hubbard M. A., Tamigney Kenfack M., Blériot Y., Gauthier C., Brett P. J., Aucoin D. P., Lanzetta R., Silipo A., Molinaro A., Burkholderia pseudomallei capsular polysaccharide recognition by a monoclonal antibody reveals key details toward a biodefense vaccine and diagnostics against melioidosis, ACS Chem. Biol.(2015) 10, 2295-2302.
    1. Metayer B. Compain G., Jouvin K., Martin-Mingot A., Bachmann C., Marrot J., Evano G., Thibaudeau S., Chemo- and Stereoselective Synthesis of Fluorinated Enamides from Ynamides in HF/pyridine: Second-Generation Approach to Potent Ureas Bioisosters, J. Org. Chem. (2015) 80, 3397-3410. (front cover)
    1. Alsarraf J., Peraudeau E., Poinot P., Tranoy-Opalinski I., Clarhaut J., Renoux B., and Papot S., A dendritic b-galactosidase-responsive folate-monomethylauristatin E conjugate, Chem. Commun. (2015), 51, 15792-15795.
    1. Simard F., Gauthier C., Chiasson E., Lavoie S., Mshvildadze V., Legault J., Pichette A., Balsacones J.-M., Hydroxycinnamoylated dihydrochalcones from Populus balsamifera buds with potent antibacterial activity, J. Nat. Prod. (2015) 78, 1147-1153.
    1. Thomas M., Opalinski I., Renoux B., Chapolin T. and Papot S., Synthesis of Benzohydroxamic Acids Glucosides and Galactosides, Carbohydrate Chemistry: Proven Synthetic Method (2015) 3 (20), 159-169.
    1. Tuan A. T., Jagadeesh Y., Luo B., Auberger N., Désiré J., Nakagawa S., Kato A., Zhang Y., Sollogoub M., Blériot Y., Synthesis of pyrrolidines-based analogues of aminosugars as N-acetyl glucosaminidase inhibitors, Carbohydr. Res. (2015) 409, 56-62.
    1. Cendret V., Legigan T., Mingot A., Thibaudeau S., Adachi I.,Forcella M., Parenti P., Bertrand J., Becq F., Norez C., Désiré J., Kato A., Blériot Y., Synthetic deoxynojirimycin derivatives bearing a thiolated, fluorinated or unsaturated N-alkyl chain: identification of potent α-glucosidase and trehalase inhibitors as well as F508del-CFTR correctors, Org. Biomol. Chem. (2015) 13, 10734-10744.
    1. Unione L., Xu B., Diaz D., Martin-Santamaria S., Poveda A., Sardinha J., Rauter A.-P., Blériot Y., Zhang Y., Canada F. J., Sollogoub M., Jimenez Barbero J., Conformational Plasticity in Glycomimetics: Fluorocarbamethyl-L-idopyranosides Mimic the Intrinsic Dynamic Behaviour of Natural Idose Rings, Chem.Eur. J. (2015) 21, 10513-10521.
    1. Laroussarie A., Barycza B., Andriamboavonjy H., Tamigney Kenfack M., Blériot Y., Gauthier C., Synthesis of the tetrasaccharide repeating unit of the β-Kdo-containing exopolysaccharide from Burkholderia pseudomallei and B. cepacia complex, J. Org. Chem. (2015) 80, 10386-10396.
    1. Denis I., El Bahhaj F., Collette F., Delatouche R., Gueugnon F., Pouliquen D., Pichavant L., Heroguez V., Gregoire M., Bertrand P., Blanquart C., Histone deacetylase inhibitor-polymer conjugate nanoparticles for acid-responsive drug delivery, Eur. J. Med. Chem. (2015) 95, 369-376.
    1. Trouiller A.-J., Hébié S.., El Bahhaj F., Napporn T. W., Bertrand P., Chemistry for oncotheranostic gold nanoparticles, Eur. J. Med. Chem. (2015) 99, 92-112.
  1. Michel B. Y, Cuendet M., Barthes N.P.F, Burger A., Bertrand P., Martinet N. Détection des modifications de la méthylation de l’ADN et de la chromatine, Revue Francophone des Laboratoires (2015), 473, 21-28.


    1. Balbous A., Renoux B., Cortes U., Milin S., Guilloteau K., Legigan T., Rivet P., Boissonnade O., Martin S., Tripiana C., Wager M., Bensadoun R.-J., Papot S., Karayan-Tapon L. Selective release of a cyclopamine glucuronide prodrug towards stem-like cancer cell inhibition in glioblastoma, Mol. Cancer Ther. (2014) 13, 2159-2169.
    1. Blériot Y., Tran A. T., Prencipe G., Jagadeesh Y, Auberger N. Zhu S. , Gauthier C., Zhang Y., Désiré J. , Idachi I., Kato A. Sollogoub M., Synthesis of 1,2-trans 2-acetamido-2-deoxy-homoiminosugars, Org. Lett.(2014) 16, 5516-5519.
    1. Blériot Y., Auberger N., Jagadeesh Y., Gauthier C., Prencipe G., Tran A. T. , Marrot J., Désiré J., Yamamoto A., Kato A., Sollogoub M., Synthesis of 1,2-cis homoiminosugars derived from GlcNAc and GalNAc exploiting a β-aminoalcohol skeletal rearrangement, Org. Lett.(2014) 16, 5512-5515.
    1. Carré G., Carreyre H., Ourdraogo M., Becq F., Bois P., Thibaudeau S., Vandebrouck C., Bescond J. The hypotensive agent dodoneine inhibits L-type Ca2+ current with negative inotropic effect on rat heart, Eur. J. Pharmacol. (2014) 728, 119-127.
    1. Désiré J., Mondon M., Fontelle N., Nakagawa S., Hirokami Y., Adachi I., Iwaki R., Fleet G.W.J., Alonzi D.S., Twigg G., Butters D., Bertrand J., Cendret V., Becq F., Norez C., Marrot J., Kato A., Blériot Y., N- and C-Alkylation of seven-membered iminosugars generate potent glucocerebrosidase inhibitors and F508del-CFTR correctors, Org. Biomol. Chem. (2014) 12, 8977-8996.
    1. El Bahhaj F., Dekker F. J., Martinet N., Bertrand P. Delivery of Epidrugs, Drug Discovery Today (2014) 19, 1337-1352.
    1. El Bahhaj F., Désiré J., Blanquart C., Martinet N., Zwick V., Simoës-Pires C., Cuendet M., Gregoire M., Bertrand P., Superacid and thiol-ene reactions for access to psammaplin analogues with HDAC inhibition activities, Tetrahedron (2014) 70, 9702-9708.
    1. Eppe G., Cavarano A., Désiré J., Vincent S.P., Synthesis of fluorinated exo-glycals mediated by Selectfluor, Carbohydrate Chemistry: Proven Synthetic Methods (2014) 2, 85-96.
    1. Gauthier C., Chassagne P., Theillet F.-X., Guerreiro C., Thouron F., Nato F., Delepierre M., Sansonetti P.J., Phalipon A., Mulard L. A. Non-stoichiometric O-acetylation of Shigella flexneri 2a O-specific polysaccharide: synthesis and antigenicity, Org. Biomol. Chem. (2014) 12, 4218-4232.
    1. Gueugnon F., Cartron P.-F., Charrier C., Bertrand P., Fonteneau J.-F., Gregoire M., Blanquart C. New histone deacetylases inhibitors improve cisplatin antitumor properties against thoracic cancer cells, Oncotarget (2014) 12, 4504-4514.
    1. Houillé B., Papon N., Boudesocque L., Bourdeaud E., Besseau S., Courdavault V., Enghenard-Guieiffier C., Delanoue G., Guérin L., Bouchara J-P., Clastre M., Giglioli-Guivarc’h, Guillard J., Lanoue A., Antifungal Activity of Resveratrol Derivatives against Candida Species, J. Nat. Prod. (2014) 77, 1658–1662.
    1. Maaliki C., Gauthier C., Massinon O., Sagar R., Vincent S. P., Blériot Y. Conformationally restricted glycoside derivatives as mechanistic probes and/or inhibitors of sugar processing enzymes and receptors, Carbohydr. Chem. (2014) 40, 418-444.
    1. Patzel K.A., Yardeni T., Le Poëc-Celic E., Leoyklang P., Dorward H., Alonzi D.S., Kukushkin N.V., Xu B., Zhang Y., Sollogoub M., Blériot Y., Gahl W.A., Huizing M., Butters T.D. Non-specific build-up of glycosphingolipids in GNE myopathy, J. Inh. Metab. Disorders (2014) 37, 297-308.
    1. Picard S., Lecornue F., Bashiardes G., Synthesis of Unique Analogues of the Ergoline Skeleton Using Intramolecular [3+2] Cycloaddition, Synlett (2014) 1106-1110.
    1. Sylla B., Gauthier C., Fleury P.-Y., Legault J., Lavoie S., Mshvildadze V., Muzashvili T., Kemertelidze E., Pichette A. Isolation of a new disaccharide nucleoside from Helleborus caucasicus: structure elucidation and total synthesis of hellecaucaside A and its β-anomer, Carbohydr. Res. (2014) 398, 80-89.
    1. Tamigney Kenfack M., Blériot Y., Gauthier C. Intramolecular aglycon delivery enables the synthesis of 6-deoxy-β-D-manno-heptosides as fragments of Burkholderia pseudomallei and Burkholderia mallei capsular polysaccharide, J. Org. Chem. (2014) 79, 4615-4634.
    1. Theunissen C., Métayer B., Henry N., Compain G., Marrot J., Martin-Mingot A., Thibaudeau S., Evano G. Keteniminium ion-initiated cascade cationic polycyclisation, J. Am. Chem. Soc. (2014) 136, 12528-12531, 2014. (Front cover + highlight)
    1. Tranoy-Opalinski I., Legigan T., Barat R., Clarhaut J., Thomas M., Renoux B., Papot S. b-glucuronidase-responsive prodrugs for selective cancer chemotherapy: An update, Eur. J. Med. Chem. (2014) 74, 302-313.
    1. Wang B., Zaborova E., Guieu S., Petrillo M., Guitet M., Blériot Y., Ménand M., Zhang Y., Sollogoub M. Site-directed hexa-hetero-functionalisation of an archetypic C6-symmetric concave cycle, -cyclodextrin, Nature Commun. (2014) 5, 5354.
    1. Xu B., Unione L., Sardinha J., Wu S., Ethève-Quelquejeu M., Pilar Rauter A., Blériot Y., Zhang Y., Martín-Santamaría S., Diaz D., Jiménez-Barbero J., Sollogoub M. Gem-difluoro-carbadisaccharides: restoring the exo-anomeric effect, Angew. Chem. Int. Ed. (2014) 53, 9597-9602.
    1. 68. Iza D., El Bahhaj F., Floraine C., Delatouche R., Gueugnon F., Pouliquen D., Pichavant L., Heroguez V., Gregoire M., Bertrand P., Blanquart C., Vorinostat–Polymer Conjugate Nanoparticles for Acid-Responsive Delivery and Passive Tumor Targeting, Biomacromolecules (2014) 15, 4534-4543.
  1. Christodoulou M. S., Thomas A., Poulain S., Vidakovic M., Lahtela-Kakkonen M., Matulis D., Bertrand P., Bartova E., Blanquart C., Mikros E., Fokialakis N., Passarella D., Benhida R., Martinet N., Can we use the epigenetic bioactivity of caloric restriction and phytochemicals to promote healthy ageing? MedChemComm (2014) 5, 1804-182.


    1. Ajas A., Bertrand P., Lemée L., Queffelec A. Stratigraphy and Palaeopedology of the Palaeolithic Cave Site of Combe-Saunière, Southwest France, Geoarchaeology 28 (2013) 432-449.
    1. Carreyre H., Coustard J-M., Carré G., Vandebrouck C., Bescond J., Ouédraogo M., Marrot J., Vullo D., Supuran C.T., Thibaudeau S. Natural product hybrid and its superacid synthesized analogues: Dodoneine and its derivatives show selective inhibition of carbonic anhydrase isoforms I, III, XIII and XIV”, Bioorg. Med. Chem. (2013) 21, 3790-3794.
    1. Clarhaut J., Fraineau S., Guilhot J., Peraudeau E., Tranoy-Opalinski I., Thomas M., Renoux B., Randriamalala E., Bois P., Chatelier A., Monvoisin A., Cronier L., Papot S., Guilhot F. A Galactosidase-Responsive Doxorubicin-Folate Conjugate for Selective Targeting of Acute Myelogenous Leukemia Blasts, Leukemia Res. (2013) 37, 948-955.
    1. Collette F., Delatouche R., Blanquart C., Gueugnon F., Grégoire M., Bertrand P., Héroguez V. An easy and effective method to produce functionalized particles for cellular uptake, J. Polym Sci. Part A: Polym. Chem. (2013) 51, 176–189.
    1. Compain G., Bonneau C., Martin-Mingot A., Thibaudeau S. Selective Anti-Markovnikov Cyclization and Hydrofluorination2 Reaction in Superacid HF/SbF5: A Tool in the Design of Nitrogen-Containing (Fluorinated) Polycyclic Systems, J. Org. Chem. (2013) 78, 4463-4472.
    1. Compain G., Martin-Mingot A., Maresca A., Thibaudeau S., Supuran C.T. Superacid synthesis of halogen containing N-subtituted-4-aminobenzenesulfonamides: New selective tumor-associated carbonic anhydrase inhibitors, Bioorg. Med. Chem. (2013) 21, 1555-1563.
    1. Delatouche R., Denis I., Grinda M., El Bahhaj F., Baucher E., Collette F., Heroguez V., Grégoire M., Blanquart C., Bertrand P. Design of pH responsive clickable prodrugs applied to histone deacetylases inhibitors: a new strategy for anticancer therapy, Eur. J. Pharm. Biopharm. (2013) 85, 862-872.
    1. Grinda M., Legigan T., Clarhaut J., Peraudeau E., Tranoy-Opalinski I., Renoux B., Thomas M., Guilhot F., Papot S. An Enzyme-Responsive System Programmed for the Double Release of Bioactive Molecules through an Intracellular Chemical Amplification Process, Org. Biomol. Chem. (2013) 11, 7129-7133
    1. Gueugnon F., Denis I., Pouliquen D., Collette F., Delatouche R., Héroguez V., Grégoire M., Bertrand P., Blanquart C. Nanoparticles produced by ring-opening metathesis polymerization using norbornenyl-poly(ethylene oxide) as a ligand-free generic platform for highly selective in vivo tumor targeting, Biomacromolecules (2013) 14, 2396-2402.
    1. Howe J.D., Smith N., Marvin L.J., Ardes-Guillot N., Désiré J., Baron A., Blériot Y., Sollogoub M., Vauzeilles B., Alonzi D.S, T.D. Butters, Novel imino sugar α-glucosidase inhibitors as antiviral drugs, Bioorg. Med. Chem. (2013) 21, 4831-4838.
    1. Huguet M., Deborde M., Papot S., Gallard H. Oxidative decarboxylation of diclofenac by manganese oxide bed filter, Water research (2013) 47, 5400-5408.
    1. Jenkinson S.F., Best D., Saville A.W., Mui J., Nakagawa S., Kunimatsu T., Alonzi D.S., Butters T.D., Norez C., Becq F., Blériot Y., Wilson F.X.,  Weymouth-Wilson A.C., Kato A., Fleet G.W.J, C-Branched Iminosugars: -Glucosidase Inhibition by Enantiomers of isoDMDP, isoDGDP and isoDAB – L-isoDMDP Compared to Miglitol and Miglustat, J. Org. Chem. (2013) 78, 7380-7397 (front cover/featured article).
    1. Legigan T., Clarhaut J., Renoux B., Tranoy-Opalinski I., Monvoisin A., Jayle C., Alsarraf J., Thomas M., Papot S., Synthesis and biological evaluations of a monomethylauristatin E glucuronide prodrug for selective cancer chemotherapy, Eur. J. Med. Chem. (2013) 67, 75-80.
    1. Legros V., Vanhaverbeke C., Souard F., Len C., Désiré J. -Cyclodextrin-glycerol dimers: synthesis and NMR conformational analysis, Eur. J. Org. Chem. (2013) 13, 2583-2590.
    1. Metayer B., Mingot A., Vuollo D., Supuran C.T., Thibaudeau S. New superacid synthesized (fluorinated) tertiary benzenesulfonamides acting as selective hCA IX inhibitors: toward a new mode of carbonic anhydrase inhibition by sulfonamides, Chem. Commun. (2013) 49, 6015-6017 (Front cover).
    1. Métayer B., Martin-Mingot A., Vullo D., Supuran C.T., Thibaudeau S. Superacid synthesized tertiary benzenesulfonamides and benzofuzed sultams act as selective hCA IX inhibitors: toward understanding a new mode of inhibition by tertiary sulfonamides, Org. Biomol. Chem. (2013) 43, 7540-7549 DOI:10.1039/C3OB41538D.
    1. Mondon M., Hur S., Vadlamani G., Rodrigues P., Madden Z., Oliver A., Mark B., Vocadlo D., Blériot Y., Selective trihydroxyazepane NagZ inhibitors increase sensitivity of Pseudomonas aeruginosa to -lactams, Chem. Commun. (2013) 49, 10983-10985.
    1. Mondon M., Lecornué F., Guillard J., Nakagawa S., Kato A., Blériot Y. Total synthesis and glycosidase inhibition profile of (-)-adenophorine, (-)-1-epi-adenophorine, and analogs obtained by skeletal rearrangement of seven-membered iminosugars, Bioorg. Med. Chem. (2013) 21, 4803-4812.
    1. Ouédraogo M., Da F.L., Fabré A., Konaté K., Dibala C.I., Carreyre H., Thibaudeau S., Coustard J.-M., Vandebrouck C., Bescond J., Belemtougri R.G. Evaluation of the Bronchorelaxant, Genotoxic, and Antigenotoxic Effects of Cassia alata L., Evidence-Based Complementary and Alternative Medicine (2013) article ID 162651.
    1. Vidal P., Roldós V., Del Carmen Fernández-Alonso M., Blériot Y., Cañada F.J, André S., Gabius H-J., Jiménez-Barbero J., Espinosa J-F, Martín-Santamaría S. Conformational selection in glycomimetics. Human galectin-1 only recognizes syn- type conformations of 1,3-linked lactose and its C-glycosyl derivative, Chem. Eur. J. (2013) 19, 14581-14590.
  1. Zaborova E., Guitet M., Prencipe G., Blériot Y., Ménand M., Sollogoub M. Unexpected Double Bank Shot of Diisobutylaluminium Hydride for Triple Functionalisation of -Cyclodextrin, Angew. Chem. Ed. Int. (2013) 52, 639-644.


    1. Amorim L., Marcello F., Désiré J., Sollogoub M., Jimenez-Barbero J., Blériot Y. Synthesis and conformational analysis of bicyclic mimics of - and -D-glucopyranosides adopting the biologically relevant 2,5B conformation, Carbohydr. Res. (2012) 361, 219-224. DOI:10.1016/j.carres.2012.07.005
    1. Boucle S., Guillard J. Synthesis of analogues of Makaluvamine A, Heterocycles (2012) 85 (3), 677-688. DOI: 10.3987/COM-11-12414
    1. Collette F., Héroguez V., Blanquart C., Gueugnon F., Grégoire M., Mondon M., Delatouche R., Len C., Bertrand P. Development of triazolyl-based pH responsive releasing systems. Proceedings of 7th Paul Walden Symposium, Riga, Latvian J. Org. Chem. 51 (2012) 41-8.
    1. Compain G., Martin-Mingot A., Frapper G., Bachmann C., Thibaudeau S. Anti-Markovnikov additions to N-allylic derivatives involving ammonium-carbenium superelectrophiles, Chem. Commun. (2012) 48 (47), 5877-5879. DOI: 10.1039/c2cc32246c
    1. Compain G., Jouvin K., Martin-Mingot A., Evano G., Marrot J., Thibaudeau S. Stereoselective hydrofluorination of ynamides: a straightforward synthesis of novel α-fluoroenamides, Chem. Comm. (2012) 48, 5196-5198. DOI: 10.1039/C2CC31768K
    1. Das I., Désiré J., Manvar D., Baussanne I., V. Pandey V.N. and Decout J-L., A Peptide Nucleic Acid–Aminosugar Conjugate Targeting Transactivation Response Element of HIV-1 RNA Genome Shows a High Bioavailability in Human Cells and Strongly Inhibits Tat-Mediated Transactivation of HIV-1 Transcription, J. Med. Chem. (2012) 55, (13) 6021-6032. DOI: 10.1021/jm300253q
    1. Delatouche R., Bachmann C., Frapper G., Bertrand P. Extending Triazolyl-Based Release under Mildly Acidic Conditions To Give Aniline Derivatives, Synthesis (2012) 44, 1090-1094.
    1. Deschamp J., Mondon M., Nakagawa S., Kato A., Alonzi D.S., Butters T.D., Zhang Y., Sollogoub M., Blériot Y. Seven-membered 1N-iminosugar homologs: synthesis and glycosidase inhibition of D-manno- and L-gulo-like tri- and tetrahydroxylated azepanes, Bioorg. Med. Chem. (2012) 20, 641-649. doi:10.1016/j.bmc.2010.09.053
    1. Farran D., Bertrand P. Hammet constants effects in microwave cascade etherification-cyclization-Krapcho reaction to access [2,3]-dihydrobenzofuran-3-ones from salicylic derivatives, Synth. Commun. (2012) 42, 989-1001.
    1. Fernandes A., Viterisi A., Aucagne V., Leigh D.A., Papot S. Second generation specific-enzyme-activated rotaxane propeptides, Chem.Commun. (2012) 48, 2083-2085. DOI: 10.1039/c2cc17458h
    1. Foureau E., Clastre M., Millerioux Y., Simkin A.J., Cornet L ., Dutilleul C., Besseau S., Marais E., Melin C., Guillard J., Crèche J., Giglioli-Guivarc’h N., Courdavault V., Papon N. A TRP5/5-Xuoroanthranilic acid counter-selection system for gene disruption in Candida guilliermondii, Current Genetics (2012) 58, 245-254. DOI 10.1007/s00294-012-0377-3
    1. Geffroy-Rodier C., Buch A., Sternberg R., Papot S. Gas chromatography-mass spectrometry of hexafluoroacetone derivatives: First time utilization of a gaseous phase derivatizing agent for analysis of extraterrestrial amino acids, Journal of Chromatography A 1245 (2012) 158-166. DOI: 10.1016/j.chroma.2012.04.062
    1. Grinda M., Clarhaut J., Renoux B., Tranoy-Opalinski I., Papot S. A self-immolative dendritic glucuronide prodrug of doxorubicin, MedChemCom. (2012) 3, 68-70 (Hot article). DOI: 10.1039/c1md00193k
    1. Guitet M., Adam de Beaumais S., Zhang Y., Blériot Y., Ménand M., Sollogoub M. Post functionalisation of diversely benzylated cyclodextrins through chemoselective O-debenzylation at position 3 using Et3SiH-I2, a consequence of the Sorrento meeting, Carbohydr. Res. (2012) 356, 278-281. doi:10.1016/j.carres.2011.12.002
    1. Legigan T., Clarhaut J., Renoux B., Tranoy-Opalinski I., Monvoisin A., Berjeaud J-M., Guilhot F., Papot S. Synthesis and antitumor efficacy of a β-glucuronidase-responsive albumin-binding prodrug of doxorubicin, J. Med. Chem. (2012) 55, 4516-4520. DOI: 10.1021/jm300348r
    1. Legigan T., Clarhaut J., Tranoy-Opalinski I., Monvoisin A., Renoux B., Thomas M., Lepape A., Lerondel S., Papot S. The First Generation of β-Galactosidase-Responsive Prodrugs Designed for the Selective Treatment of Solid Tumours in Prodrug Monotherapy, Angew. Chem. Int. Ed. (2012) 51, 11606-11610 (Inside cover). DOI: 10.1002/anie.201204935
    1. Le Roux J., Gallard H., Croue J.P., Papot S., Deborde M. NDMA Formation by Chloramination of Ranitidine: Kinetics and Mechanism, Environmental Science & Technology 46 (2012) 11095-11103. DOI: 10.1021/es3023094
    1. Li H., Zhang Y., Favre S., Vogel P., Sollogoub M., Blériot Y. Synthesis of branched seven-membered 1-N-iminosugars and their evaluation as glycosidase inhibitors, Carbohydr. Res. (2012) 356, 110-114. doi:10.1016/j.carres.2011.10.039
    1. Martin-Mingot A., Compain G., Liu F., Jouannetaud M-P., Bachmann C., Frapper G., Thibaudeau S. Dications in superacid HF/SbF5: When Superelectrophilic Activation Makes Possible Fluorination and/or C-H Bond Activation, J. Fluor. Chem. (2012) 134, 56-62. DOI: 10.1016/j.jfluchem.2011.04.022
    1. Martin-Mingot A., De Oliveira Vigier K., Jérôme F., Thibaudeau S. High efficiency of superacid HF/SbF5 for the selective decrystallization/depolymerization of cellulose to glucose, Org. Biomol.Chem. (2012) 10, 2521-2524. DOI: 10.1039/c2ob07143f
    1. Martinet N., Michel B., Bertrand P., Benhida R. Small molecules DNA methyl transferases inhibitors, MedChemComm. (2012) 3, 263.
    1. Mondon M., Fontelle N., Désiré J., Lecornue F., Guillard J., Marrot J., Blériot Y., Access to D- and L-Imino-Sugar C-Glycosides from a D-Gluco-Derived 6-Azidolactol Exploiting a Ring Isomerization/Alkylation Strategy, Org. Lett. (2012) 14, 870-873. DOI 10.1021/ol203385w
    1. Perez-Castells J., Fontanella M., Arda A., Canada F.J., Sollogoub M., Blériot Y., Jimenez-Barbero J. Conformational analysis of seven-membered 1-N-iminosugars by NMR and molecular modeling, New. J. Chem. (2012) 36, 1008-1013. DOI: 10.1039/C2NJ20967E
    1. Sardinha J., Rauter A.P., Sollogoub M., Blériot Y. Synthesis of gem-difluorocarbasugars by TIBAL induced rearrangement, Carbohydrate Chemistry : Proven Methods (2012) 2, (14), 129-135.
    1. Trapencieris P., Strazdina J., Bertrand P. Synthesis of small and medium size monocyclic hydroxamic acids, Chemistry of Heterocyclic Compounds (2012) 48, 833-855.
  1. Vuong S., Brondel N., Len C., Papot S., Renoux B. Formal synthesis of TMC-69-6H via a one-pot enantioselective domino proline-mediated aldol/olefin homologation procedure, Tetrahedron (2012) 68, 433-439. DOI: 10.1016/j.tet.2011.11.025

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