Scientific Articles

2016

Pires Ado R, Lecerf-Schmidt F, Guragossian N, Pazinato J, Gozzi GJ, Winter E, Valdameri G, Veale A, Boumendjel A, Di Pietro A, Pérès B, New, highly potent and non-toxic, chromone inhibitors of the human breast cancer resistance protein ABCG2. Eur J Med Chem. 2016 Oct 21;122:291-301.

Rocheblave L, Rolland de Ravel M, Monniot E, Tavenard J, Cuilleron CY, Grenot C, Radix S, Matera EL, Dumontet C, Walchshofer N. Deoxycholic acid derivatives as inhibitors of P-glycoprotein-mediated multidrug efflux. Steroids, 2016 Dec;116:5-12.

Baiceanu E, Nguyen KA, Gonzalez-Lobato L, Nasr R, Baubichon-Cortay H, Loghin F, Le Borgne M, Chow L, Boumendjel A, Peuchmaur M, Falson P. 2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2. Eur. J. Med. Chem. 2016  Oct 21;122:408-18.  

Goudard A, Lalande L, Bertin C, Sautereau M, Le Borgne M, Cabelguenne D. Sleep disorders and therapeutic management: a survey in a French population of prisoners. J Correct Health Care. 2016 in press.

Belguedj R, Lamera E, Bouraiou A, Bouaziz Z, Chibani A. Methyl 3-(Quinolin-2-yl)indolizine-1-carboxylate. Molbank. 2015 Dec 28;2016(1):M883.

Coupat-Goutaland B, Régoudis E, Besseyrias M, Mularoni A, Binet M, Herbelin P, Pélandakis M. Population Structure in Naegleria fowleri as Revealed by Microsatellite Markers. PLoS One. 2016 Apr 1;11(4):e0152434.

Le Borgne M, Haidar S, Duval O, Wünsch B, Jose J. Pharmaceuticals (Basel). 1st Joint European Conference on Therapeutic Targets and Medicinal Chemistry (TTMC 2015). 2016 Jan;9(1):1-41.

Do CV, Faouzi A, Barette C, Farce A, Fauvarque MO, Colomb E, Catry L, Berthier-Vergnes O, Haftek M, Barret R, Lomberget T. Synthesis and biological evaluation of thiophene and benzo[b]thiophene analogs of combretastatin A-4 and isocombretastatin A-4: A comparison between the linkage positions of the 3,4,5-trimethoxystyrene unit. Bioorg Med Chem Lett. 2016 Jan 1;26(1):174-80.

Alchab F, Sibille E, Ettouati L, Bana E, Bouaziz Z, Mularoni A, Monniot E, Bagrel D, Jose J, Borgne ML, Chaimbault P. Screening of indeno[1,2-b]indoloquinones by MALDI-MS: a new set of potential CDC25 phosphatase inhibitors brought to light, J Enzyme Inhib Med Chem. 2016,  Jun 30:1-8.

Zeinyeh W, Radix S, Terreux R, Chemelle JA, Walchshofer N. Unsymmetrical α, ω-end-functionalized oligo(cyclohexylidenes): efficient synthesis and conformational analysis. Tetrahedron. 2016 Jul 7;72(27-28):4032-4038.

Gaubert A, Jame P, Bordes C, Clément Y, Guibert S, Batteau M, Lomberget T, Anchisi A, Lantéri P, Casabianca H. Determination of surfactant bio‐sourced origin by isotope‐ratio mass spectrometry. Rapid Communications in Mass Spectrometry. 2016 May 15;30(9):1108-14.

Bollacke A, Nienberg C, Borgne ML, Jose J. Toward selective CK2alpha and CK2alpha' inhibitors: Development of a novel whole-cell kinase assay by Autodisplay of catalytic CK2alpha'. J Pharm Biomed Anal. 2016 Jan 8. pii: S0731-7085(16)30011-5.

2015

Le Borgne M, Haidar S, Duval O, Wünsch B, Jose J. 1st Joint European Conference on Therapeutic Targets and Medicinal Chemistry (TTMC 2015). Pharmaceuticals (Basel). 2015 Dec 26;9(1).

Lamera E, Benzerka S, Bouraiou A, Bouacida S, Merazig H, Chibani A, Le Borgne M, Bouaziz Z. Crystal structure of 13-phenyl-2,3,4,13-tetrahydro-1 H -indazolo[1,2- b ]phthalazine-1,6,11-trione. Acta Cryst. 2015;E71:o1036-o1037.

Do CV, Faouzi A, Barette C, Farce A, Fauvarque MO, Colomb E, Catry L, Berthier-Vergnes O, Haftek M, Barret R, Lomberget T. Synthesis and biological evaluation of thiophene and benzo[b]thiophene analogs of combretastatin A-4 and isocombretastatin A-4: A comparison between the linkage positions of the 3,4,5-trimethoxystyrene unit. Bioorg Med Chem Lett. 2016 Jan 1;26(1):174-80.

Lecerf-Schmidt F, Haudecoeur R, Peres B, Ferreira Queiroz MM, Marcourt L, Challal S, Ferreira Queiroz E, Sotoing Taiwe G, Lomberget T, Le Borgne M, Wolfender JL, De Waard M, Robins RJ, Boumendjel A. Biomimetic synthesis of Tramadol. Chem Commun (Camb). 2015 Oct 4;51(77):14451-3.

Gozzi GJ, Bouaziz Z, Winter E, Daflon-Yunes N, Honorat M, Guragossian N, Marminon C, Valdameri G, Bollacke A, Guillon J, Pinaud N, Marchivie M, Cadena SM, Jose J, Le Borgne M, Di Pietro A. Phenolic indeno[1,2-b]indoles as aBcg2-selective potent and non-toxic inhibitors stimulating basal aTPase activity. Drug Des Devel Ther. 2015;9:1–15. 

Bouraiou A, Bouacida S, Merazig H, Chibania A, Bouaziz Z. Crystal structure of 13-(2-methoxy- phenyl)-3,4-dihydro-2H-indazolo[1,2-b]- phthalazine-1,6,11(13H)-trione. Acta Cryst. 2015;E71:o604–o605.

Bouaziz Z, Issa S, Gentili J, Gratz A, Bollacke A, Kassack M, Jose J, Herfindal L, Gausdal G, Døskeland SO, Mullié C, Sonnet P, Desgrouas C, Taudon N, Valdameri G, Di Pietro A, Baitiche M, Le Borgne M. Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds. J Enzyme Inhib Med Chem. 2015 Apr;30(2):180-8.

Belhani B, Berredjem M, Le Borgne M, Bouaziz Z, Lebreton J, Aouf N-E. A one-pot three-component synthesis of novel α-sulfamidophosphonates under ultrasound irradiation and catalyst-free conditions. RSC Adv., 2015:5:39324-39329.

Gratz A, Bollacke A, Stephan S, Nienberg C, Le Borgne M, Götz C, Jose J. Functional display of heterotetrameric human protein kinase CK2 on Escherichia coli: a novel tool for drug discovery. Microb Cell Fact. 2015 Jun 3;14:74.  

Alchab F, Ettouati L, Bouaziz Z, Bollacke A, Delcros JG, Gertzen CGW, Gohlke H, Pinaud N, Marchivie M, Guillon J, Fenet B, Jose J, Le Borgne M. Synthesis, Biological Evaluation and Molecular Modeling of Substituted Indeno[1,2-b]indoles as Inhibitors of Human Protein Kinase CK2. Pharmaceuticals 2015;8:279-302.

de Ravel MR, Alameh G, Melikian M, Mahiout Z, Emptoz-Bonneton A, Matera EL, Lomberget T, Barret R, Rocheblave L, Walchshofer N, Beltran S, El Jawad L, Mappus E, Grenot C, Pugeat M, Dumontet C, Le Borgne M, Cuilleron CY. Synthesis of new steroidal inhibitors of p-glycoprotein-mediated multidrug resistance and biological evaluation on k562/r7 erythroleukemia cells. J Med Chem. 2015 Feb 26;58(4):1832-45.

Marminon C, Nacereddine A, Bouaziz Z, Nebois P, Jose J, Le Borgne M. Microwave-assisted oxidation of indan-1-ones into ninhydrins. Tetrahedron Lett. 2015 Apr 1;56(14):1840-42.

Gozzi GJ, Bouaziz Z, Nacereddine A, Marminon C, Winter E, Valdameri G, Zeinyeh W, Bollacke A, Jose J, Guillon J, Lacoudre A, Pinaud N, Cadena SM, Le Borgne M, Di Pietro A. Converting Potent Indeno[1,2-b]indole Inhibitors of Protein Kinase CK2 into Selective Inhibitors of the Breast Cancer Resistance Protein ABCG2. J Med Chem. 2015 Jan 8;58(1):265-77.

Neyra C, Paladino J, Le Borgne M.
Mechanisms of depolymerization and activation of a polysialic acid and its tetramer by hydrogen peroxide. Carbohydr Polym. 2015 Jan 22;115:494-501.

2014


Defaux J, Antoine M, Logé C, Le Borgne M, Schuster T, Seipelt I, Aicher B, Teifel M, Günther E, Gerlach M, Marchand P. Discovery of (7-aryl-1,5-naphthyridin-2-yl)ureas as dual inhibitors of ERK2 and Aurora B kinases with antiproliferative activity against cancer cells. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3748-52. 

Defaux J, Antoine M, Le Borgne M, Schuster T, Seipelt I, Aicher B, Teifel M, Günther E, Gerlach M, Marchand P. Discovery of 7-aryl-substituted (1,5-naphthyridin-4-yl)ureas as Aurora kinase inhibitors.
ChemMedChem. 2014 Jan;9(1):217-32.

Bourezg Z, Cartiser N, Ettouati L, Guillon J, Lacoudre A, Pinaud N, Le Borgne M, Fessi H. Structural elucidation of two photolytic degradation products of tetrabenazine. J Pharm Biomed Anal. 2014 Jan 3;91C:138-43.

Neyra C, Paladino J, Le Borgne M. Oxidation of sialic acid using hydrogen peroxide as a new method to tune the reducing activity. Carbohydr Res. 2014 Jan 14;386C:92-8.

2013

Agusti G, Bourgeois S, Cartiser N, Fessi H, Le Borgne M, Lomberget T. A safe and practical method for the preparation of 7α-thioether and thioester derivatives of spironolactone. Steroids. 2013 Jan;78(1):102-7.

Perret F, Marminon C, Zeinyeh W, Nebois P, Bollacke A, Jose J, Parrot-Lopez H, Le Borgne M. Preparation and characterization of CK2 inhibitor-loaded cyclodextrin nanoparticles for drug delivery. Int J Pharm. 2013 Jan 30;441(1-2):491-8.

Nguyen TTB, Lomberget T, Tran NC, Barret R. Synthesis of (Z) isomers of benzoheterocyclic derivatives of combretastatin A-4: a comparative study of several methods. Tetrahedron. 2013 March 11;69(10):2336-47.

Guillon J, Le Borgne M, Rimbault C, Moreau S, Savrimoutou S, Pinaud N, Baratin S, Marchivie M, Roche S, Bollacke A, Pecci A, Alvarez L, Desplat V, Jose J. Synthesis and biological evaluation of novel substituted pyrrolo[1,2-a]quinoxaline derivatives as inhibitors of the human protein kinase CK2. Eur J Med Chem. 2013 Jul;65:205-22.

Boumendjel A, Sotoing Taïwe G, Ngo Bum E, Chabrol T, Beney C, Sinniger V, Haudecoeur R, Marcourt L, Challal S, Ferreira Queiroz E, Souard F, Le Borgne M, Lomberget T, Depaulis A, Lavaud C, Robins R, Wolfender JL, Bonaz B, De Waard M. Occurrence of the Synthetic Analgesic Tramadol in an African Medicinal Plant. Angew Chem Int Ed Engl. 2013 Nov 4; 52(45):11780-84.

Rongved P, Kirsch G, Bouaziz Z, Jose J, Le Borgne M. Indenoindoles and cyclopentacarbazoles as bioactive compounds: Synthesis and biological applications. Eur J Med Chem. 2013 Sep 16;69:465-79.

Alchab F, Fenet B, Le Borgne M, Jose J, Pinaud N, Guillon J, Ettouati L. 1H and 13C NMR assignments of bioactive indeno[1,2-b]indole-10-one derivatives. Magn Reson Chem. 2013 Dec;51(12):837-41.

2012


Hundsdörfer C, Hemmerling HJ, Götz C, Totzke F, Bednarski P, Le Borgne M, Jose J. Indeno[1,2-b]indole derivatives as a novel class of potent human protein kinase CK2 inhibitors. Bioorg Med Chem. 2012 Apr 1;20(7):2282-9.

Hundsdörfer C, Hemmerling HJ, Hamberger J, Le Borgne M, Bednarski P, Götz C, Totzke F, Jose J. Novel indeno[1,2-b]indoloquinones as inhibitors of the human protein kinase CK2 with antiproliferative activity towards a broad panel of cancer cell lines. Biochem Biophys Res Commun. 2012 Jul 20;424(1):71-5.

Nachtergaele L, Callejon S, Abdayem R, Nguyen TTB, Lomberget T, Barret R, Haftek M. Microtubule depolymerisation with anticancer drugs: combretastatin A-4 analogues. Exp Dermatol. 2012 Sep;21(9):E7.

Zeinyeh W, Mahiout Z, Radix S, Lomberget T, Dumoulin A, Barret R, Grenot C, Rocheblave L, Matera EL, Dumontet C, Walchshofer N. Progesterone-adenine hybrids as bivalent inhibitors of P-glycoprotein-mediated multidrug efflux: design, synthesis, characterization and biological evaluation. Steroids. 2012 Oct;77(12):1177-91.

Nguyen TTB, Lomberget T, Tran NC, Colomb E, Nachtergaele L, Thoret S, Dubois J, Guillaume J, Abdayem R, Haftek M, Barret R. Synthesis and biological evaluation of novel heterocyclic derivatives of combretastatin A-4. Bioorg Med Chem Lett. 2012 Dec 1;22(23):7227-31.