IRHC HDRMise à jour le 20/12/2021
Brevets / Publications / Communications
Publications
95. Dao V.H., Ourliac-Garnier I., Logé C., McCarthy F.O., Bach S., da Silva T.G., Denevault-Sabourin C., Thiéfaine J., Baratte B., Robert T., Gouilleux F., Brachet-Botineau M., Bazin M.-A., Marchand P. 2021. Dibenzofuran Derivatives Inspired from Cercosporamide as Dual Inhibitors of Pim and CLK1 Kinases. Molecules, 26, 6572. https://doi.org/10.3390/molecules26216572.
94. Choudhary B. S., Sukanya, Mehta P., Bach S., Ruchaud S., Robert T., Josselin B., Filipek S., Malik R. 2021. Discovery of thiazolidin-4-one analogue as selective GSK-3β inhibitor through structure based virtual screening. Bioorganic & Medicinal Chemistry Letters. Volume 52 (128375). https://doi.org/10.1016/j.bmcl.2021.128375.
93. Pieterse L., Beteck R.M., Baratte B., Jesumorotia O., Robert T., Ruchaud S., Bach S., Legoabe L. J. 2021. Synthesis and biological evaluation of selected 7H-pyrrolo[2,3-d]pyrimidine derivatives as novel CDK9/CyclinT and Haspin inhibitors. Chemico-Biological Interactions. https://doi.org/10.1016/j.cbi.2021.109643.
92. Ahmadu A.A., Delehouzé C., Haruna A., Mustapha L., Lawal B.A., Udobre A., Baratte B., Triscornia C., Autret A., Robert T., Bulinski J.C., Rousselot M., Simoes Eugénio M., Dimanche-Boitrel M., Petzer J.P., Legoabe L.J., Bach, S. 2021. Betulin, a Newly Characterized Compound in Acacia Auriculiformis Bark, is a Multi-target Protein Kinase Inhibitor. Molecules 2021, 26, 4599. https://doi.org/10.3390/molecules26154599. This article was previously published as preprint. Preprints 2021, 2021060115 (doi: 10.20944/preprints202106.0115.v1).
91. Qhobosheane M., Beteck R. M., Baratte B., Robert T., Ruchaud S., Bach S., Legoabe L.J. 2021. Exploration of 7-azaindole-coumaranone hybrids and their analogues as protein kinase inhibitors. Chemico-Biological Interactions, Available online 25 April 2021, 109478. https://doi.org/10.1016/j.cbi.2021.109478
90. Lassagne F.*, Sims J.M., Erb W., Mongin O., Richy N., El Osmani N., Fajloun Z.*, Picot L., Thiery V., Robert T., Bach S.*, Dorcet V., Roisnel T. and Mongin F.* 2021. Thiazolo[5,4‐f]quinoxalines, oxazolo[5,4‐f]quinoxalines and pyrazino[b,e]isatins: synthesis from 6‐aminoquinoxalines and properties. Eur. J. Org. Chem. https://doi.org/10.1002/ejoc.202100362
89. Oyallon B., Brachet-Botineau M., Logé C., Robert T., Bach S., Ibrahim S., Raoul W., Croix C., Berthelot P., Guillon J., Pinaud N., Gouilleux F., Viaud-Massuard M-C., Denevault-Sabourin C. 2021. New Quinoxaline Derivatives as Dual Pim-1/2 Kinase Inhibitors: Design, Synthesis and Biological Evaluation. Molecules. 26(4):867. https://doi.org/10.3390/molecules26040867
88. Juillet C., Ermolenko L., Boyarskaya D., Baratte B., Josselin B., Nedev H., Bach S., Iorga B., Bignon J., Ruchaud S., Al-Mourabit A. 2021. From Synthetic Simplified Marine Metabolite Analogues to New Selective Allosteric Inhibitor of Aurora B Kinase. Journal of Medicinal Chemistry. 64(2), 1197-1219. https://doi.org/10.1021/acs.jmedchem.0c02064
87. Brahmaiah D., Bhavani A., Aparna P., Kumar N., Solhi H., Le Guevel R., Baratte B., Ruchaud S., Bach S., Jadav S., Reddy C., Roisnel T., Mosset P., Levoin N. and Grée R. 2021. Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase. Bioorganic & Medicinal Chemistry. DOI: https://doi.org/10.1016/j.bmc.2020.115962
86. Delehouzé C., Comte A., Hauteville M., Goekjian P., Dimanche-Boitrel M-T., Rousselot M.* and Bach S.* 2020. Nigratine as first-in-class dual inhibitor of necroptosis and ferroptosis regulated cell death. Preprint. BioRxiv 2020.12.15.422885; doi: https://doi.org/10.1101/2020.12.15.422885.
85. Elie J., Feizbakhsh O., Desban N., Josselin B., Baratte B., Bescond A., Duez J., Fant X., Bach S., Marie D., Place M., Ben Salah S., Chartier A., Berteina-Raboin S., Chaikuad A., Knapp S., Carles F., Bonnet P., Buron F., Routier S. and Ruchaud S. 2020. Design of new disubstituted imidazo[1,2-b]pyridazine derivatives as selective Haspin inhibitors. Synthesis, binding mode and anticancer biological evaluation, Journal of Enzyme Inhibition and Medicinal Chemistry, 35:1, 1840-1853, DOI: 10.1080/14756366.2020.1825408.
84. Wilde M., Arzur D., Baratte B., Lefebvre D., Robert T., Roisnel T., Le Jossic-Corcos C., Bach S.*, Corcos L.* and Erb W.* 2020. Regorafenib analogues and their ferrocenic counterparts: synthesis and biological evaluation. The article was first published on 10 Nov 2020. New J. Chem., https://doi.org/10.1039/D0NJ05334A.
83. Princival I., Princival J., da Silva E., Lima S., Carregos J., de Lucenaa A., Halwass F., Franc J., Ferreir L., Hernandes M., Saraiv K., Peixoto K., Baratte B., Robert T., Bach S., Gomes D., Paiva D., Marchand P., Rodrigues M. and da Silva T. 2021. Streptomyces hygroscopicus UFPEDA 3370: a valuable source of the potent cytotoxic agent nigericin and its evaluation against human colorectal cancer cells. Chemico-Biological Interactions. doi.org/10.1016/j.cbi.2020.109316.
82. Bazin A., Cojean S., Pagniez F., Bernadat G., Cavé C., Ourliac-Garnier I., Nourrisson M.-R., Morgado C., Picot C., Leclercq O., Baratte B., Robert T., Späth G.F., Rachidi N., Bach S., Loiseau P.M., Le Pape P. and Marchand P. 2021. In vitro identification of imidazo[1,2-a]pyrazine-based antileishmanial agents and evaluation of L. major casein kinase 1 inhibition. European Journal of Medicinal Chemistry. Available online 23 October 2020, 112956. https://doi.org/10.1016/j.ejmech.2020.112956.
81. Tuescher J. M., Tailfeathers D., Kernéis S.M., Baratte B., Ruchaud S., Bach S., Pouny I., Sautel F., and Golsteyn R.M. 2020. The Canadian prairie plant Thermopsis rhombifolia contains luteolin, a flavone that inhibits Cyclin dependent kinase 9 and arrest cells in the G1-phase of the cell cycle. The Journal of Natural Health Product Research. Vol. 2 No. 2 (2020): July-December 2020, doi.org/10.33211/jnhpr.12.
80. Esvan Y., Josselin B., Baratte B., Bach S., Ruchaud S., Anizon F., Giraud F. and Moreau P. 2020. Synthesis and kinase inhibitory potencies of new pyrido[3,4-g]quinazolines substituted at the 8-position. ARKIVOC, 2020(7), DOI: 10.24820/ark.5550190.p011.268.
79. Cousseau A., Siano R., Probert I., Bach S. and Mehiri M. 2020. Marine Dinoflagellates as source of new bioactive structures. Studies in Natural Products Chemistry (Bioactive Natural Products), ISBN 9780128179055. ELSEVIER SCIENCE PUBLISHERS – AMSTERDAM. Vol. 65, 125-171. https://doi.org/10.1016/B978-0-12-817905-5.00004-4.
78. Pieterse L., Legoabe L., Beteck R., Josselin B., Bach S. and Ruchaud S. 2020. Synthesis and biological evaluation of selected 7-azaindole derivatives as CDK9/Cyclin T and Haspin inhibitors. Medicinal Chemistry Research. Accepted: 7 May 2020. doi.org/10.1007/s00044-020-02560-1.
77. Bouattour A., Fakhfakh M., Abid S., Paquin L., Le Guével R., Charlier T., Ruchaud S., Bach S., Bazureau J.-P. and Ammar H. 2020 Synthesis of new 2-phenylamino-4H-chromene-3-carbonitrile derivatives and their effects on tumor cell lines and against protein kinases. Internat. J. Org. Chem. 10, 88-103. doi: 10.4236/ijoc.2020.102006.
76. Bach S., Colas P. et Blondel M. 2020. La levure modèle et outil… aussi pour la recherche thérapeutique. Médecine & Sciences. m/s n° 5, vol. 36, 504-513, https://doi.org/10.1051/medsci/2020077.
75. Ibrahim N., Bonnet P., Briona J.D., Peyrata J.F., Bignonc J., Levaiquec H., Josselin B., Robert T., Colas P., Bach S., Messaoudia S., Alamia M., Hamze A. 2020. Identification of a new series of Flavopiridol-like structures as kinase inhibitors with high cytotoxic potency. European Journal of Medicinal Chemistry. Volume 199, 1 August 2020, 112355, doi.org/10.1016/j.ejmech.2020.112355.
74. Benchekroun M., Ermolenko L., Tran M.Q., Vagneux A., Nedev H., Delehouzé C., Souab M., Baratte B., Josselin B., Iorga B., Ruchaud S., Bach S.* and Al-Mourabit A.* 2020. Discovery of Simplified Benzazole Fragments Derived From The Marine Benzosceptrin B as Necroptosis Inhibitors Involving The Receptor Interacting Protein Kinase-1. European Journal of Medicinal Chemistry. 201: 112337, 2020 Sep 01, 10.1016/j.ejmech.2020.112337.
73. Qhobosheane MA., Legoabe LJ., Josselin B., Bach S., Ruchaud S., Petzer J., Beteck R. 2020. Synthesis and evaluation of 7-azaindole derivatives bearing benzocycloalkanone motifs as protein kinase inhibitors [published online ahead of print, 2020 Mar 31]. Bioorg Med Chem. 2020;115468. doi:10.1016/j.bmc.2020.115468.
72. Robert T., Johnson J.L., Guichaoua R., Yaron T.M., Bach S., Cantley L.C. and Colas P. 2020. Development of a CDK10/CycM in vitro Kinase Screening Assay and Identification of First Small-Molecule Inhibitors. Front. Chem., 27 February 2020. DOI: 10.3389/fchem.2020.00147.
71. From simple quinoxalines to potent oxazolo[5,4-f]quinoxaline inhibitors of glycogen-synthase kinase 3 (GSK3). 2019. Lassagne F., Duguépéroux C., Roca C., Pérez C., Martinez A., Baratte B., Robert T., Ruchaud S., Bach S.*, Erb W., Roisnel T. and Mongin F. Org. Biomol. Chem., DOI: 10.1039/C9OB02002K.
70. Nascimento da Cruz A.C., Brondani D.J., I´talo de Santana T., Oliveira da Silva L., da Oliveira Borba E.F., de Faria A.R., Ferreira Cavalcanti de Albuquerque J., Piessard S., Matos Ximenes R., Baratte B., Bach S., Ruchaud S., Bezerra Mendonça Junior F.J., Bazin M.-A., Montenegro Rabello M., Hernandes M.Z., Marchand P. and Gonçalves da Silva T. 2019. Biological Evaluation of Arylsemicarbazone Derivatives as Potential Anticancer Agents. Pharmaceuticals, 12, 169.
69. Mokhtari Brikci-Nigassa N., Nauton L., Moreau P., Mongin O., Duval R., Picot L., Thiéry V., Souab M., Ruchaud S., Bach S.*, Guevel R., Bentabed-Ababsa G., Erb W., Roisnel T., Dorcet V., Mongin F. 2019. Functionalization of 9-thioxanthone at the 1-position: from arylamino derivatives to [1]benzo(thio)pyrano[4,3,2-de]benzothieno[2,3-b]quinolines of biological interest, Bioorganic Chemistry, 103347, doi.org/10.1016/j.bioorg.2019.103347.
68. Nguyen TN., Feizbakhsh O., Sfecci E., Baratte B., Delehouzé C., Garcia A., Moulin C., Colas P., Ruchaud S.*, Mehiri M.*, and Bach S. * 2019. Kinase-Based Screening of Marine Natural Extracts Leads to the Identification of a Cytotoxic High Molecular Weight Metabolite from the Mediterranean Sponge Crambe tailliezi. Mar Drugs. 2019 Oct 9;17(10). pii: E569. doi: 10.3390/md17100569.
67. Ziane S., Mazari M.M., Safer A.M., Sad El Hachemi Amar A., Ruchaud S., Baratte B. and Bach S. 2019. Comparison between Conventional and Nonconventional Methods for the Synthesis of Some 2-Oxazolidinone Derivatives and Preliminary Investigation of Their Inhibitory Activity Against Certain Protein Kinases. Russian Journal of Organic Chemistry. July 2019, Volume 55, Issue 7 (1061–1069). doi.org/10.1134/S1070428019070248.
66. Sartini S, Levati E., Maccesi M., Guerra M., Spadoni G., Bach S., Benincasa M., Scocchi M., Ottonello S., Rivara S. and Montanini B. 2019. New Antimicrobials Targeting Bacterial RNA Polymerase Holoenzyme Assembly Identified with an in Vivo BRET-Based Discovery Platform. ACS Chem Biol. 2019 Jul 30. doi: 10.1021/acschembio.9b00178.
65. Khaldoun K., Safer A., Boukabcha N., Dege N., Ruchaud S., Souab M., Bach S., Chouaih A. and Saidi-Besbes S. 2019. Synthesis and evaluation of new isatin-aminorhodanine hybrids as PIM1 and CLK1 kinase inhibitors. Journal of Molecular Structure. 1192 (82-90). ISSN 0022-2860. doi.org/10.1016/j.molstruc.2019.04.122.
64. Zeinyeh W., Esvan Y. J., Josselin B., Baratte B., Bach S., Nauton L., Théry V., Ruchaud S., Anizon F., Giraud F. and Moreau P. 2019. Kinase inhibitions in pyrido[4,3-h] and [3,4-g]quinazolines: Synthesis, SAR and molecular modeling studies. Bioorganic & Medicinal Chemistry. ISSN 0968-0896. doi.org/10.1016/j.bmc.2019.04.005.
63. Oukoloff K., Coquelle N., Bartolini M., Naldi M., Le Guevel R., Bach S., Josselin B., Ruchaud S., Catto M., Pisani L., Denora N., Iacobazzi R.M., Silman I., Sussman J.L., Buron F., Colletier J.-P., Jean L., Routier S. and Renard P.-Y. 2019. Design, biological evaluation and X-ray crystallography of nanomolar multifunctional ligands targeting simultaneously acetylcholinesterase and glycogen synthase kinase-3. European Journal of Medicinal Chemistry, doi.org/10.1016/j.ejmech.2018.12.063.
62. Motuhi S.-E., Feizbakhsh O., Foll-Josselin B., Baratte B., Delehouzé C., Cousseau A., Fant X., Bulinski J.C., Payri C.E., Ruchaud S., Mehiri M.* and Bach S.* 2019. Neurymenolide A, a Novel Mitotic Spindle Poison from the New Caledonian Rhodophyta Phacelocarpus neurymenioides. Mar. Drugs, 17, 93.
61. Tazarki H., Zeinyeha W., Esvana, Y.J., Snapp K., Chatterjee D., Schröder M., Joerger A. C., Khiarib J., Josselin B., Baratte B., Bach S., Ruchaud S., Anizona F., Giraud F. and Moreau P. 2019. New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis. European Journal of Medicinal Chemistry, https://doi.org/10.1016/j.ejmech.2019.01.052.
60. Masłyk, M., Janeczko, M., Martyna, A., Czernik, S., Tokarska-Rodak, M., Chwedczuk, M., Foll-Josselin, B., Ruchaud, S., Bach, S., Demchuk, O.M. and Kubiński, K. 2019. The Anti-Candida albicans Agent 4-AN Inhibits Multiple Protein Kinases. Molecules, 24, 153. doi.org/10.3390/molecules24010153.
59. Lassagne F., Langlais T., Caytan E., Limanton E., Paquin L.*, Boullard M., Courtel C., Curbet I., Gédéon C., Lebreton J., Picot L.*, Thiery V., Souab M., Baratte B., Ruchaud S., Bach S.*, Roisnel T. and Mongin F. 2018. From quinoxaline, pyrido[2,3-b]pyrazine and pyrido[3,4-b]pyrazine to pyrazino-fused carbazoles and carbolines. Molecules. doi: 10.3390/molecules23112961.
58. Serive B. and Bach S. 2018. Marine Pigment Diversity: Applications and Potential. Chapter #20 of the textbook «Blue Technologies: production and use of marine molecules». Edited by Stéphane La Barre and Stephen Bates, Wiley VCH, Weinheim, Germany, pages 643-681, ISBN: 978-3-527-34138-2.
57. Winfield H.J., Cahill M.M., O'Shea K.D., Pierce L.T., Robert T., Ruchaud S., Bach S., Marchand P. and McCarthy FO. 2018. Synthesis and anticancer activity of novel bisindolylhydroxymaleimide derivatives with potent GSK-3 kinase inhibition. Bioorg Med Chem. 2018 Aug 7;26(14):4209-4224. doi: 10.1016/j.bmc.2018.07.012. Epub 2018 Jul 9.
56. Dao V.H., Ourliac-Garnier I., Bazin M.-A., Jacquot C., Baratte B., Ruchaud S., Bach S., Grovel O., Le Pape P. and Marchand P. 2018. Benzofuro[3,2-d]pyrimidines inspired from cercosporamide CaPkc1 inhibitor: synthesis and evaluation of fluconazole susceptibility restoration. Bioorganic & Medicinal Chemistry Letters. BMCL-D-18-00505. DOI:10.1016/j.bmcl.2018.05.044.
55. Oyallon B., Brachet-Botineau M., Logé C., Bonnet P., Souab M., Robert T., Ruchaud S., Bach S., Berthelot P., Gouilleux F., Viaud-Massuard M.-C. and Denevault-Sabourin C. 2018. Structure-based design of novel quinoxaline-2-carboxylic acids and analogues as Pim-1 inhibitors. Eur. J. Med. Chem. 154:101-109. doi: 10.1016/j.ejmech.2018.04.056.
54. von Mässenhausen A., Tonnus W., Himmerkus N., Parmentier S., Saleh D., Rodriquez D., Ousingsawat J., Ang R.L., Weinberg J.M., Sanz A.B., Ortiz A., Zierleyn A., Becker J.U., Baratte B., Desban N., Bach S., Schiessl I.M., Nogusa S., Balachandran S., Anders H.J., Ting A.T., Bleich M., Degterev A., Kunzelmann K., Bornstein S.R., Green D.R., Hugo C. and Linkermann A. 2018. Phenytoin inhibits necroptosis. Cell Death Dis., 9(3):359. doi: 10.1038/s41419-018-0394-3.
53. Brikci-Nigassa N.M., Bentabed-Ababsa G.*, Erb W., Chevallier F., Picot L.*, Vitek L., Fleury A., Thiéry V., Souab M., Robert T., Ruchaud S., Bach S.*, Roisnel T. and Mongin F.*. 2018. 2-Aminophenones, a common precursor to N-aryl isatins and acridines endowed with bioactivities. Tetrahedron (TET-D-18-00014R1), in press. DOI information: 10.1016/j.tet.2018.02.038.
52. Hamza-Reguig S., Bentabed-Ababsa G.*, Domingo L.R., Ríos-Gutiérrez M., Philippot S., Fontanay S., Duval R. E.*, Ruchaud S., Bach S.*, Roisnel T.* and Mongin F.* 2017. A combined experimental and theoretical study of the thermal [3+2] cycloaddition of carbonyl ylides with activated alkenes. J. Mol. Struct. doi.org/10.1016/j.molstruc.2017.12.052.
51. Ahmadu A. A., Agunu A., Nguyen T-N-D., Baratte B., Foll-Josselin B., Ruchaud S., Serive B. and Bach S. 2017. Constituents of Acacia nilotica Delile with Novel Kinase inhibitory activity. Planta Medica International Open. 4: e108–e113.
50. Bazureau J-P., Bouattour A., Fakhfakh M., Abid S., Ammar H., Paquin L., Le Guével R., Corlu, A., Ruchaud S. and Bach S. 2017. Reactivity under Microwave Irradiation of 2-Amino 4H-chromene-3-carbonitrile as Tool for the Construction of Potential Bioactive Derivatives. In Proceedings of the 3rd Int. Electron. Conf. Med. Chem., 1–30 November 2017; Sciforum Electronic Conference Series, Vol. 3, 2017 ; doi:10.3390/ecmc-3-04709.
49. Delehouzé C., Leverrier-Penna S., Le Cann F., Comte A., Jacquard-Fevai M., Delalande O., Desban N., Baratte B., Gallais I., Faurez F., Bonnet MC., Hauteville M., Goekjian PG., Thuillier, R., Favreau F., Vandenabeele P., Hauet T., Dimanche-Boitrel MT*., and Bach S*. 2017. 6E11, a new highly selective inhibitor of Receptor-Interacting Protein Kinase 1, protects cells against cold hypoxia-reoxygenation injury. Sci. Rep.; 7(1):12931. doi: 10.1038/s41598-017-12788-4.
48. Hedidi M., Maillard J., Erb W., Lassagne F., Halauko Y. S., Ivashkevich O. A., Matulis V. E., Roisnel T., Dorcet V., Hamze M., Fajloun Z., Baratte B., Ruchaud S., Bach S.* and Bentabed-Ababsa G.* and Mongin F.* 2017. Fused systems based on 2-aminopyrimidines: synthesis combining deprotolithiation-in situ zincation with N-arylation reactions and biological properties. Eur. J. Org. Chem. 10.1002/ejoc.201701004.
47. Kim J., Brown C.M., Kim M. K., Burrows E. H., Bach S., Lun D. S., Falkowski P. G. 2017. The effect of cell cycle arrest on intermediate metabolism in the marine diatom Phaeodactylum tricornutum. Proc Natl Acad Sci U S A. DOI: 10.1073/pnas.1711642114.
46. Le Cann F., Delehouzé C., Penna-Leverrier S., Filliol A., Comte A., Delalande O., Desban N., Baratte B., Gallais I., Piquet-Pellorce C., Faurez F., Bonnet M., Mettey Y., Goekjian P., Samson M., Vandenabeele P., Bach S.* and Dimanche-Boitrel M-T.* 2017. Sibiriline, a new small chemical inhibitor of Receptor-Interacting Protein Kinase 1, prevents immune-dependent hepatitis. FEBS Journal, 284(18):3050-3068, DOI: 10.1111/febs.14176.
45. Ali Bouattour A., Fakhfakh M., Abid S., Paquin L., Le Guével R., Corlu A., Ruchaud S., Bach S., Ammar H. and Bazureau J.-P. 2017. Microwave-assisted practical synthesis of 4-imino-3-phenyl-3,4-dihydro-1Hchromeno[2,3-d]pyrimidine-2(5H)-thione derivatives and exploration of their biological activities. Arkivoc 2017, part iv, 291-302.
44. Navarri M., Bondon A., Pottier S., Bach S., Baratte B., Ruchaud S., Barbier G., Burgaud G. and Fleury Y. 2017. Bioactive metabolites from the deep subseafloor fungus Oidiodendron griseum UBOCC-A-114129. Mar. Drugs., Apr 7;15(4). pii: E111. doi: 10.3390/md15040111.
43. Corbel C., Sartini S., Levati E., Colas P., Maillet L., Couturier C., Montanini B.* and Bach S.* 2017. Screening for protein-protein interaction inhibitors using a Bioluminescence Resonance Energy Transfer (BRET) based assay in yeast. SLAS Discovery (formerly Journal of Biomolecular Screening), 22(6):751-759, doi:1:2472555216689530.
42. Sklepari M., Lougiakis N., Papastathopoulos A., Pouli N., Marakos P., Myrianthopoulos V., Robert T., Bach S., Mikros E. and Ruchaud S. 2017. Synthesis, docking study and kinase inhibitory activity of a number of new substituted pyrazolo[3,4-c]pyridines. Chem Pharm Bull (Tokyo). 65(1):66-81. doi: 10.1248/cpb.c16-00704.
41. Daniilides K., Lougiakis N., Evangelidis T., Kostakis I.K., Pouli N., Marakos P., Mikros E., Skaltsounis AL., Bach S., Baratte B., Ruchaud S., Karamani V., Papafotika A., Christoforidis S., Argyros O., Kouvari E. and Tamvakopoulos C. 2016. Discovery of new aminosubstituted pyrrolopyrimidines with antiproliferative activity against breast cancer cells and investigation of their effect towards the PI3Kα enzyme. Anticancer Agents Med Chem. 2016 Dec 7. [Epub ahead of print]
40. Ambeu N'ta C., Déliko Dago C-D., Coulibaly W-K., Békro Y-A., Mamyrbekova-Békro JA., Foll-Josselin B., Defontaine A., Delehouzé C., Bach S., Ruchaud S., Le Guével R., Corlu A., Jéhan P., Lambert F., Le Yondre N. and Bazureau J-P. 2016. Microwave synthesis of new 3-(3-aminopropyl)-5-arylidene-2-thioxo-1,3-thiazolidine-4-ones as potential Sr/Thr proteine kinase inhibitors. Medicinal Chemistry Research. 25, accepted for publication. DOI: 10.1007/s00044-016-1719-3.
39. Hedidi M., Erb W., Bentabed-Ababsa G., Chevallier F., Picot L., Thiéry V., Bach S., Ruchaud, S., Roisnel T., Dorcet, V. and Mongin, F. 2016. Synthesis of N-pyridyl azoles using a deprotometalation-iodolysis-N-arylation sequence and evaluation of their antiproliferative activity in melanoma cells. Tetrahedron 2016, 72, 6467-6476. DOI: 10.1016/j.tet.2016.08.056.
38. Lawson M., Rodrigo J., Baratte B., Robert T., Delehouzé C., Lozach O., Ruchaud S., Bach S., Brion J.-D., Alami M., Hamze A. 2016. Synthesis, biological evaluation and molecular modeling studies of Imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors. Eur J Med Chem. 2016 Nov 10;123:105-14. doi: 10.1016/j.ejmech.2016.07.040. Epub 2016 Jul 21.
37. Bazin M.A., Rousseau B., Marhadour S., Tomasoni C., Evenou P., Piessard S., Vaisberg A.J., Ruchaud S., Bach S., Roussakis C., Marchand P. 2016. Discovery of Novel (Imidazo[1,2-a]pyrazin-6-yl)ureas as Antiproliferative Agents Targeting P53 in Non-small Cell Lung Cancer Cell Lines. Anticancer Res., 36(4):1621-1630.
36. Motuhi S-E., Mehiri M., Payri C. E., La Barre S.* and Bach S.* 2016. Marine natural products from New Caledonia – a review. Mar Drugs. 2016 Mar 16;14(3). pii: E58. doi: 10.3390/md14030058.
35. Moine E., Dimier-Poisson I., Enguehard-Gueiffier C., Logé C., Pénichon M., Moiré N., Delehouzé C., Foll-Josselin B., Ruchaud S., Bach S., Gueiffier A., Debierre-Grockiego F. and Denevault-Sabourin C. 2015. Development of new highly potent imidazo[1,2-b]pyridazines targeting Toxoplasma gondii calcium-dependent protein kinase 1. Eur J Med Chem. 2015 Oct 9; 105:80-105. doi: 10.1016/j.ejmech.2015.10.004.
34. Marquise N., Tai Nguyen T., Chevallier F., Picot L., Thiéry V., Lozach O., Bach S., Ruchaud S., Mongin F. 2015. Azine and Diazine Functionalization using 2,2,6,6-Tetramethylpiperidino-Based Lithium-Metal Combinations. Application to the Synthesis of 5,9-Disubstituted Pyrido[3’,2’:4,5]pyrrolo[1,2-c]pyrimidines. Synlett 09/2015; DOI:10.1055/s-0035-1560496.
33. Marchand P., Bazin M.A., Pagniez F., Rivière G., Bodero L., Marhadour S., Nourrisson M-R., Picot C., Ruchaud S., Bach S., Baratte B., Sauvain M., Castillo Pareja D., Vaisberg A., Le Pape P. 2015. Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines. Eur. J. Med. Chem, 103, 381-395. doi: 10.1016/j.ejmech.2015.09.002.
32. Déliko Dago C.D., N'Ta Ambeu C., Coulibaly W.K., Bekro Y.A., Mamyrbekova J., Defontaine A., Baratte B., Bach S., Ruchaud S., Le Guével R., Ravache M., Corlu A., Bazureau J-P. 2015. Synthetic Development of New 3-(4-Arylmethylamino)butyl-5-arylidene-rhodanines Under Microwave Irradiation and their Effects on Tumor Cell Lines and against Protein Kinases. Molecules. 20, 12412-12435; doi:10.3390/molecules200712412.
31. Corbel C., Zhang B., Le Parc A., Baratte B., Colas P., Couturier C., Kosik S. K., Landrieu I., Le Tilly V., and Bach S.* 2015. Tamoxifen Inhibits CDK5 Kinase Activity by Interacting with p35/p25 and Modulates the Pattern of Tau Phosphorylation. Chemistry & Biology 22 (4), 472-482. *corresponding author.
30. Baratte B., Serive B. et Bach S*. 2015. Le criblage à Roscoff: une recherche d'inhibiteurs de kinases tournée vers la mer. Médecine & Sciences. 31(5); 538-545. *corresponding author.
29. Hochard A., Reininger L., Ruchaud S. and Bach S*. 2014. High-Throughput Screening of marine resources. Chapter of the textbook “Outstanding Marine Molecules”. Outstanding Marine Molecules, edited by Stéphane La Barre (Editor), Jean-Michel Kornprobst (Editor). ISBN: 978-3-527-33465-0. 536 pages. April 2014, Wiley-Blackwell. *corresponding author.
28. Abida H., Ruchaud S., Rios L., Humeau A., Probert I., De Vargas C., Bach S.*, Bowler C.* 2013. Bio-prospecting the Ocean’s Plankton. Mar. Drugs, 11, 4594-4611; doi:10.3390/md11114594. *corresponding authors.
27. Corbel, C., Wang, Q., Bousserouel, H., Hamdi, A., Zhang, B., Lozach, O., Ferandin, Y., Tan, V.B., Guéritte, F., Colas, P., Couturier, C. and Bach, S*. 2011. First BRET-based screening assay performed in budding yeast leads to the discovery of CDK5/p25 interaction inhibitors. Biotechnol J. 6(7):860-870. *corresponding author.
26. Zhang, B., Corbel, C., Guéritte, F., Couturier, C., Bach, S. and Tan, V.B. 2011. An in silico approach for the discovery of CDK5/p25 interaction inhibitors. Biotechnol J. 2011 Jul;6(7):871-81.
25. Menn B., Bach S., Blevins T.L., Campbell M., Meijer L. and Timsit S. 2010. Delayed treatment with systemic (S)-roscovitine provides neuroprotection and inhibits in vivo CDK5 activity increase in animal stroke models. PLoS One. 5(8):e12117.
24. Gug F., Oumata N., Tribouillard-Tanvier D., Voisset C., Desban N., Bach S., Blondel M. and Galons H. 2010. Synthesis of Conjugates of 6-Aminophenanthridine and Guanabenz two structurally unrelated prion inhibitors for the determination of their cellular targets by affinity chromatography. Bioconjug Chem. 21:279-288.
23. Sasvari Z., 1, Bach S., Blondel M. and Nagy P. 2009. Inhibition of RNA recruitment and replication of an RNA virus by acridine derivatives with known anti-prion activities. PLoS One. 4(10):e7376.
22. Corbel C., Haddoub R., Guiffant D., Lozach O., Gueyrard D., Lemoine J., Ratin M., Meijer L., Bach S.* and Goekjian P.* 2009. Identification of potential cellular targets of aloisine A by affinity chromatography. Bioorgan. Med. Chem. 17(15):5572-82. *corresponding author.
21. Tribouillard-Tanvier D., Dos Reis S., Gug F., Voisset C., Beringue V., Sabate R., Kikovska E., Talarek N., Bach S., Huang C., Desban N., Saupe S. J., Supattapone S., Thuret J-Y., Chédin S., Vilette D., Galons H., Sanyal S. and Blondel M. 2008. Protein folding activity of rRNA is a selective target of two unrelated antiprion drugs. PLoS One, 3(5): e2174.
20. Tribouillard-Tanvier D., Béringue V., Desban N., Gug F., Bach S., Voisset C., Galons H., Laude H., Vilette D. and Blondel M. 2008. Antihypertensive drug Guanabenz is active in vivo against both yeast and mammalian prions. PLoS One, 3(4): e1981.
19. Bacart J., Corbel C., Jockers R., Bach S. and Couturier C. 2008. The BRET technology and its application to screening assays. Biotechnology Journal, 3:311-24.
18. Tribouillard D., Gug F., Galons H., Bach S., Saupe S.J. and Blondel M. 2007. Antiprion drugs as chemical tools to uncover mechanisms of prion propagation. Prions. 1: 48-52.
16. Iurisci I., Filipski E., Reinhardt J., Bach S., Gianella-Borradori A., Lacobelli S., Meijer L. and Lévi F. 2006. Improved tumor control through circadian clock induction by Seliciclib, a cyclin-dependent kinase inhibitor. Cancer Research 66:10720-10728.
15. Bach S., Blondel M. and Meijer L. 2006. Evaluation of CDK inhibitor selectivity: from affinity chromatography to yeast genetics. In “Monographs on enzyme inhibitors”, Volume 2. CDK inhibitors and their potential as anti-tumor agents » (E. Yue and P.J. Smith, editors). CRC Press, Taylor & Francis, chapter 5, 103- 119.
14. Bach S., Tribouillard D., Talarek N., Desban N. and Blondel M. 2006. A yeast-based assay to isolate drugs active against mammalian prions. Methods. 39:72-77.
13. Le Sourd F., Bellé R., Bach S., Boulben S., Cormier P. and Mulner-Lorillon O. 2006. Cellular coexistence of two high molecular subsets of eEF1B complex. FEBS Letters 580:2755-2760.
12. Deschamps C., Bach S., Portetelle D. and Vandenbol M. 2006. The Tre2 oncoprotein, implicated in Ewing’s sarcoma, interacts with two components of the cytoskeleton. Biotechnology letters 28:223-231.
11. Tribouillard D., Bach S., Gug F., Desban N., Beringue V., Andrieu T., Dormont D., Galons H., Laude H., Vilette D. and Blondel M. 2006. Using budding yeast to screen for anti-prion drugs. Biotechnology Journal 1: 58-67.
10. Tang L., Li MH., Cao P., Wang F., Chang WR., Bach S., Reinhardt J., Ferandin Y., Galons H., Wan Y., Gray N., Meijer L., Jiang T. and Liang DC. 2005. Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. J. Biol. Chem. 280: 31220-31229.
9. Bach S., Knockaert M., Reinhardt J., Lozach O., Schmitt S., Baratte B., Koken M., Coburn S., Tang L., Jiang T., Liang D-C., Galons H., Dierick J-F., Pinna L., Meggio F., Totzke F., Schächtele C., Lerman A., Carnero A., Wan Y., Gray N. and Meijer L. 2005. Roscovitine targets : protein kinases and pyridoxal kinase. J. Biol. Chem. 280: 31208-31219.
8. Blondel M., Bach S., Bamps S., Dobbelaere J., Wiget P., Longaretti C., Barral Y., Meijer L. and Peter M. 2005. Degradation of Hof1 by SCFGrr1 is important for actomyosin contraction during cytokinesis in yeast. EMBO Journal 24: 1440-1452.
7. Adolph S., Bach S., Blondel M., Cueff A., Moreau M., Pohnert G., Poulet S.A., Wichard T. and Zuccharo A. 2004. Cytotoxicity of diatom-derived oxylipins in organisms belonging to different phyla. J. Exp. Biol. 207:2935-2946.
6. Gug F., Bach S., Blondel M., Vierfond J-M., Martin A-S. and Galons H. 2004. A single step synthesis of 6-aminophenanthridines from anilines and 2-chlorobenzonitriles. Tetrahedron 60:4705-4708.
5. Knockaert M., Blondel M., Bach S., Leost M., Elbi C., Hager G., Nagy S., Han D., Denison M., Ffrench M., Ryan X.P., Magiatis P., Polychronopoulos P., Greengard P. Skaltsounis L. and Meijer L. 2004. Independent actions on cyclin-dependent kinases and aryl hydrocarbon receptor mediate the anti-proliferative effects of indirubins. Oncogene 23:4400-4412.
4. Wan Y., Hur W., Cho C.Y., Liu Y., Adrian F.J., Lozach O., Bach S., Mayer T., Fabbro D., Meijer L. and Gray N.S. 2004. Synthesis and target identification of hymenialdisine analogs. Chemistry and Biology 11:1-13.
3. Bach S., Talarek N., Andrieu T., Vierfond J-M., Mettey Y., Galons H., Dormont D., Meijer L., Cullin C. and Blondel M. 2003. Isolation of drugs active against mammalian prions using a yeast-based screening assay. Nature Biotechnology 21:1075-1081. Article commenté dans : Saupe S. J. 2003. New anti-prion drugs make yeast blush. Trends in Biotechnology. 21:516-519.
2. Bizimungu C., De Neve N., Burny A., Bach S., Bontemps F., Portetelle D. and Vandenbol M. 2003. Expression in a RabGAP yeast mutant of two human homologues, one of which is an oncogene. Biochem. Biophys. Res. Commun. 310:498-504.
1. Bach S., Bouchat O., Portetelle D. and Vandenbol M. 2000. Co-deletion of the yeast MSB3 and MSB4 coding regions affects bipolar budding and perturbs the organisation of the actin cytoskeleton. Yeast 16:1015-1023.
Brevets:
8. Bach S., Comte A., Delehouzé C., Dimanche-Boitrel M-T. and Goekjian P. (2021). Inhibitors of Ferroptosis Regulated Cell Death. Request for grant of a European patent, n°21305085.9 – 1112 (filed on January 25, 2021).
7. Bach S., Dimanche-Boitrel M-T., Delehouzé C. and Hauet T. (2016) -EP1630636.3. Natural Product Derivatives for Inhibiting cellular necroptosis, ferroptosis and Oxytosis. Request for grant of a European patent, n°1630636.3 (filed on October 18, 2016). International patent application under the PCT/EP2017/076638 (filed on October 18, 2017).
6. Bach S., Comte A., Delehouzé C., Dimanche-Boitrel M-T., Goekjian P. and Mettey Y. (2015) – EP 3 362 449 – US 10,426,758. Sibiriline derivatives for use for preventing and/or treating disorders associated with cellular necroptosis. Request for grant of a European patent, n°15306624.6, filed on October 13, 2015. International patent application under the PCT/EP2016/074638 (filed on October 13, 2016). US extension published October, 1st 2019 (n° 10426758).
5. Bach S., Comte A., Delehouzé C., Dimanche-Boitrel M-T. and Goekjian P. (2015) – EP 3 362 450 – US 10,457,678. N1- and N7-substituted sibiriline derivatives and their use as inhibitor of cellular necroptosis. Request for grant of a European patent, n°15306623.8 filed on October 13, 2015. International patent application under the PCT/EP2016/074637 (filed on October, 13, 2016).
4. Corbel C., Couturier, C., Guerrite, F., Zhu-Wang, Q., Bousserouel, H. and Bach, S. Chemical inhibitors of protein-protein interactions targeting protein kinases and their use in human therapy: Androstan derivatives / Composés inhibiteurs d’interactions protéine-protéine ciblant les protéines kinases et leurs applications biologiques: Dérivés d’androstane. Patent Application FR 10/04627, 29 November 2010. Abandoned.
3. Corbel C., Couturier, C. and Bach, S. Chemical inhibitors of protein-protein interactions targeting protein kinases and their use in human therapy: Tamoxifen and derivatives / Inhibiteurs d’interactions protéine-protéine ciblant les protéines kinases et leurs applications biologiques: le tamoxifène et ses dérivés (2010). Patent Application FR 10/04625, 29 November 2010. Abandoned.
2. Blondel, M., Bach, S., Vilette, D. and Beringue, V. Use of Chlorine Guanabenz derivatives for treating prion-based diseases. (2006) Request of a European patent application. EP n° 06 291 548.3 filed by CNRS on october, 04 2006. Abandoned.
1. Bach, S., Talarek, N., Vierfond, J.-M., Mettey, Y., Cullin, C. and Blondel, M. Screening molecules with anti-prion activity: kits, methods and screened molecules. (2002, 2003) French patent application: FR00213022 et FR0308289 filed on october 18, 2002 and on july 7, 2003. PCT extension on october 20, 2003 (PCT/FR2003/03101).