Créé(e) 16/06/2015 Mis à jour 10/02/2017


Microwave synthesis of new 3-(3-aminopropyl)-5-arylidene-2-thioxo-1,3-thiazolidine-4-ones as potential Sr/Thr proteine kinase inhibitors. 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 Medicinal Chemistry Research. 25, accepted for press, DOI:10.1007/s00044-016-1719-3.

Synthesis of N-pyridyl azoles using a deprotometalation-iodolysis-N-arylation sequence and evaluation of their antiproliferative activity in melanoma cells. Hedidi M., Erb W., Bentabed-Ababsa G., Chevallier F., Picot L., Thiéry V., Bach S., Ruchaud, S., Roisnel T., Dorcet, V. and Mongin, F. 2016Tetrahedron 72, 6467-6476. DOI: 10.1016/j.tet.2016.08.056.

Synthesis, biological evaluation and molecular modeling studies of Imidazo[1,2-a]pyridines derivatives as protein kinase inhibitors. Lawson M., Rodrigo J., Baratte B., Robert T., Delehouzé C., Lozach O., Ruchaud S., Bach S., Brion J.-D., Alami M. and Hamze A. 2016 European Journal of Medicinal Chemistry

Discovery of Novel (Imidazo[1,2-a]pyrazin-6-yl)ureas as Antiproliferative Agents Targeting P53 in Non-small Cell Lung Cancer Cell Lines. Bazin M.A., Rousseau B., Marhadour S., Tomasoni C., Evenou P., Piessard S., Vaisberg A.J., Ruchaud S., Bach S., Roussakis C. and Marchand P. 2016 Anticancer Res

Marine natural products from New Caledonia. a review.Motuhi S-E., Mehiri M., Payri C. E., La Barre S. and Bach S. 2016  Marine Drugs.


Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors. Boulahjar R, Ouach A, Bourg S, Bonnet P, Lozach O, Meijer L, Guguen-Guillouzo  C, Le Guevel R, Lazar S, Akssira M, Troin Y, Guillaumet G, Routier S. Eur J Med Chem. 2015 Aug 28;101:274-87. 

Novel Adociaquinone Derivatives from the Indonesian Sponge Xestospongia sp.
He F, Mai LH, Longeon A, Copp BR, Loaëc N, Bescond A, Meijer L, Bourguet-Kondracki ML. Mar Drugs. 2015 Apr 28;13(5):2617-28. doi: 10.3390

10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A. Falke H, Chaikuad A, Becker A, Loaëc N, Lozach O, Abu Jhaisha S, Becker W, Jones PG, Preu L, Baumann K, Knapp S, Meijer L, Kunick C. J Med Chem. 2015 Apr 9;58(7):3131-43.

Synthesis and molecular modelling studies of 8-arylpyrido[3',2':4,5]thieno[3,2-d]pyrimidin-4-amines as multitarget Ser/Thr kinases inhibitors. Loidreau Y, Deau E, Marchand P, Nourrisson MR, Logé C, Coadou G, Loaëc N, Meijer L, Besson T Eur J Med Chem. 2015 Mar 6;92:124-34

Dispacamide E and other bioactive bromopyrrole alkaloids from two Indonesian marine sponges of the genus Stylissa. Ebada SS, Linh MH, Longeon A, de Voogd NJ, Durieu E, Meijer L, Bourguet-Kondracki ML, Singab AN, Meller WE, Proksch P. Nat Prod Res. 2015 Feb;29(3):231-8.

Tamoxifen inhibits CDK5 kinase activity by interacting with p35/p25 and modulates the pattern of tau phosphorylation. Corbel C, Zhang B, Le Parc A, Baratte B, Colas P, Couturier C, Kosik KS, Landrieu I, Le Tilly V, Bach S.  Chem Biol. 2015 Apr 23;22(4):472-82.

Tampering with cell division by using small-molecule inhibitors of CDK-CKS protein interactions. Hamdi A, Lesnard A, Suzanne P, Robert T, Miteva MA, Pellerano M, Didier B, Ficko-Blean E, Lobstein A, Hibert M, Rault S, Morris MC, Colas P. Chembiochem. 2015 Feb 9;16(3):432-9.

Screening marine resources to find novel chemical inhibitors of disease-relevant protein kinases. Baratte B, Serive B, Bach S.  Med Sci (Paris). 2015 May;31(5):538-45.

Development of new highly potent imidazo[1,2-b]pyridazines targeting Toxoplasma gondii calcium-dependent protein kinase 1. 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, Denevault-Sabourin C. Eur J Med Chem. 2015 Nov

Synthesis, antileishmanial activity and cytotoxicity of 2,3-diaryl- and 2,3,8-trisubstituted imidazo[1,2-a]pyrazines. Marchand P, Bazin MA, Pagniez F, Rivière G, Bodero L, Marhadour S, Nourrisson MR, Picot C, Ruchaud S, Bach S, Baratte B, Sauvain M, Pareja DC, Vaisberg AJ, Le Pape P. Eur J Med Chem. 2015 Oct

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. Dago CD, Ambeu CN, Coulibaly WK, Békro YA, Mamyrbékova J, Defontaine A,Baratte B, Bach S, Ruchaud S, Guével RL, Ravache M, Corlu A, Bazureau JP. Molecules. 2015 Jul 8;20(7):12412-35

Natural product extracts of the Canadian prairie plant,Thermopsis rhombifolia, have anti-cancer activity in phenotypic cell-based assays. Kernéis S, Swift LH, Lewis CW, Bruyère C, Oumata N, Colas P, Ruchaud S, Bain J, Golsteyn RM. Nat Prod Res. 2015; 29(11):1026-34. doi: 10.1080/14786419.2014.979423.


Impact of meriolins, a new class of cyclin-dependent kinase inhibitors, on malignant glioma proliferation and neo-angiogenesis. Jarry M, Lecointre C, Malleval C, Desrues L, Schouft MT, Lejoncour V, Liger F, Lyvinec G, Joseph B, Loaëc N, Meijer L, Honnorat J, Gandolfo P, Castel H. Neuro Oncol. 2014 Jun 2.

Design and Synthesis of Thiazolo[5,4-f]quinazolines as DYRK1A Inhibitors, Part I.
Foucourt A, Hédou D, Dubouilh-Benard C, Désiré L, Casagrande AS, Leblond B, Loäec N, Meijer L, Besson T. Molecules. 2014 Sep 29;19(10):15546-71. doi: 10.3390/molecules191015546.

9- and 11-substituted 4-azapaullones are potent and selective inhibitors of African trypanosoma. Maiwald F, Benítez D, Charquero D, Dar MA, Erdmann H, Preu L, Koch O, Hölscher C, Loaëc N, Meijer L, Comini MA, Kunick C. Eur J Med Chem. 2014 Aug 18;83:274-83.

Synthesis, biological evaluation and molecular modelling studies of 4-anilinoquinazoline derivatives as protein kinase inhibitors. Waiker DK, Karthikeyan C, Poongavanam V, Kongsted J, Lozach O, Meijer L, Trivedi P. Bioorg Med Chem. 2014 Mar 15;22(6):1909-15.

Several Human Cyclin-Dependent Kinase Inhibitors, Structurally Related to Roscovitine, As New Anti-Malarial Agents.Sandrine Houzé , Nha-Thu Hoang , Olivier Lozach , Jacques Le Bras , Laurent Meijer, Hervé Galons and Luc Demange. Molecules 2014, 19, 15237-15257

Synthesis and biological evaluation of tetrahydro[1,4]diazepino[1,2-a]indol-1-ones as cyclin-dependent kinase inhibitors.  Putey A, Fournet G, Lozach O, Perrin L, Meijer L, Joseph B. Eur J Med Chem. 2014 Aug 18;83:617-29

cdc-like/dual-specificity tyrosine phosphorylation-regulated kinases inhibitor leucettine L41 induces mTOR-dependent autophagy: implication for Alzheimer's disease.
Fant X, Durieu E, Chicanne G, Payrastre B, Sbrissa D, Shisheva A, Limanton E, Carreaux F, Bazureau JP, Meijer L. Mol Pharmacol. 2014 Mar;85(3):441-50.

Synthesis of new pyridazino[4,5-b]indol-4-ones and pyridazin-3(2H)-one analogs as DYRK1A inhibitors. Bruel A1, Bénéteau R1, Chabanne M1, Lozach O2, Le Guevel R3, Ravache M3, Bénédetti H4, Meijer L5, Logé C6, Robert JM. Bioorg Med Chem Lett. 2014 Sep 16.

Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors. Beniddir MA, Le Borgne E, Iorga BI, Loaëc N, Lozach O, Meijer L, Awang K, Litaudon M.
J Nat Prod. 2014 May 23;77(5):1117-22.