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Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues

Prado, Soizic Janin, Yves L. Saint-Joanis, Brigitte Brodin, Priscille Michel, Sylvie Koch, Michel Cole, Stewart T. Tillequin, Francois Bosta, Pierre-Etienne

Bioorganic & Medicinal Chemistry, 2007-3

https://doi.org/10.1016/j.bmc.2006.12.009

Sylvie MICHEL

MICHEL Sylvie

ORCID: 0000-0002-3993-4041

http://www.pharmacognosie-parisdescartes.fr/index.php/sylvie-michel-Pr

Chemical composition and biological properties of Ipomoea procumbens 10.1016/j.bjp.2018.08.010

17-OXOELLIPTICINE, A NEW ALKALOID FROM STRYCHNOS-DINKLAGEI 10.1016/S0040-4039(00)92862-4

ELLIPTICINE, MAJOR ALKALOID FROM BARK OF STRYCHNOS-DINKLAGEI 10.1021/NP50008A009

ALKALOIDS FROM THE STEM BARKS OF STRYCHNOS-DINKLAGEI 10.1021/NP50022A024

DINKLAGEINE, A NEW TYPE OF MONOTERPENE ALKALOID 10.1016/S0040-4039(01)81289-2

PLANTS OF NEW-CALEDONIA .94. MONOTERPENE ALKALOIDS OF SCAEVOLA-RACEMIGERA DANIKER 10.1002/HLCA.19850680622

ALKALOIDS FROM THE LEAVES OF STRYCHNOS-DINKLAGEI 10.1021/NP50037A015

BRAFOUEDINE AND ISOBRAFOUEDINE - NEW MINOR INDOLIC ALKALOIDS OF STRYCHNOS-DINKLAGEI 10.1021/NP50045A012

STRELLIDIMINE - THE 1ST NATURAL BIS-ELLIPTICINE ALKALOID 10.1039/C39870000229

A NOVEL SYNTHESIS OF 6-DEMETHOXYACRONYCINE 10.3987/COM-92-5981

SYNTHESIS OF NOVEL TARGETED PRO-PRODRUGS OF ANTHRACYCLINES POTENTIALLY ACTIVATED BY A MONOCLONAL-ANTIBODY GALACTOSIDASE CONJUGATE .1 10.1016/S0960-894X(00)80625-3

Synthesis and cytotoxic and antitumor activity of esters in the 1,2-dihydroxy-1,2-dihydroacronycine series 10.1021/JM9602975

Synthesis and aromatization of dihydropyrimidines structurally related to calcium channel modulators of the nifedipine-type 10.3987/COM-97-7931

Prodrugs of anthracyclines for use in antibody-directed enzyme prodrug therapy 10.1021/JM970589L

Chiral dihydroxylation of acronycine: Absolute configuration of natural cis-1,2-dihydroxy-1,2-dihydroacronycine and cytotoxicity of (1R,2R)- and (1S,2S)-1,2-diacetoxy-1,2-dihydroacronycine 10.1021/NP980420Q

Synthesis and cytotoxic activity of 11-nitro and 11-amino derivatives of acronycine and 6-demethoxyacronycine 10.1248/CPB.47.1604

Synthesis and cytotoxic and antitumor activity of benzo[b]pyrano[3,2-h]acridin-7-one analogues of acronycine 10.1021/JM990972L

Synthesis and cytotoxic activity of benzopyranoxanthone analogues of benzo[b]acronycine and psorospermine 10.1248/CPB.49.675

Induction of cyclin E and inhibition of DNA synthesis by the novel acronycine derivative S23906-1 precede the irreversible arrest of tumor cells in S phase leading to apoptosis 10.1124/MOL.60.6.1383

Structure-activity relationships in the acronycine series 10.2174/0929867023369213

Covalent binding to glutathione of the DNA-alkylating antitumor agent, S23906-1 10.1046/J.1432-1033.2003.03663.X

Structure-activity relationships and mechanism of action of antitumor benzo[b]pyrano[3,2-h]acridin-7-one acronycine analogues 10.1021/JM030790Y

A new pyranoacridone alkaloid from the bark of Medicosma subsessilis (Rutaceae) 10.1515/ZNB-2003-1213

A transesterification reaction is implicated in the covalent binding of benzo[b]acronycine anticancer agents with DNA and glutathion 10.1016/J.BMC.2003.10.056

Synthesis and cytotoxic and antitumor activity of 1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine diacid hemiesters and carbamates 10.1248/CPB.52.293

New diterpenes from Croton insularis 10.1021/NP030423P

Synthesis and cytotoxic activity of pyranocarbazole analogues of ellipticine and acronycine 10.1248/CPB.52.540

Synthesis and cytotoxic activity of benzo[c][1,7] and [1,8]phenanthrolines analogues of nitidine and fagaronine 10.1016/J.BMC.2004.04.038

Benzo[b]acronycine derivatives: a novel class of antitumor agents 10.1016/J.EJMECH.2004.05.001

New antitubulin derivatives in the combretastatin A4 series: synthesis and biological evaluation 10.1016/J.BMC.2005.02.039

Design, synthesis, and cytotoxic activity of Michael acceptors and enol esters in the benzo[b]acronycine series 10.1248/CPB.53.919

Synthesis, antitumor activity, and mechanism of action of benzo[a]pyrano[3,2-h]acridin-7-one analogues of acronycine 10.1021/JM0602007

Synthesis and biological evaluation of (3,4,5-trimethoxyphenyl)indol-3-ylmethane derivatives as potential antivascular agents 10.1016/J.BMC.2006.02.037

Synthesis and cytotoxic activity of benzo[a]pyrano[3,2-h] and [2,3-i]xanthone analogues of psorospermine, acronycine, and benzo[a]acronycine 10.1248/CPB.54.1113

Benzofuro[3,2-f][1]benzopyrans: A new class of antitubercular agents 10.1016/J.BMC.2006.03.033

Synthesis of benzo[c][1,8]phenanthrolin-6-one through cyclization of N-(isoquinol-5-yl)-2-bromo-benzamide derivatives 10.1002/JHET.5570430518

seco-cycloartane triterpenes from Gardenia aubryi 10.1021/NP060273T

Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues 10.1016/J.BMC.2006.12.009

Synthesis and cytotoxic activity of dimeric analogs of acronycine in the benzo[b]pyrano[3,2-h]acridin-7-one series 10.1248/CPB.55.734

Antimycobacterial benzofuro[3,2-f]chromenes from a 5-bromochromen-6-ol 10.1055/S-2007-966019

Synthesis and Angiotensin Converting Enzyme (ACE) inhibition activity of chalcone derivatives 10.1055/S-2007-987247

Synthesis, cytotoxic activity and mechanism of action of new Psorospermin-Acronycine analogs 10.1055/S-0028-1084793

Natural products as privileged structures for the conception of novel antimycobacterial agents 10.1055/S-0028-1084768

Design, synthesis and biological evaluation of 13-aza derivatives of benzo[b]acronycine 10.1055/S-0028-1084767

Synthesis, cytotoxic activity, and DNA binding properties of antitumor cis-1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine cinnamoyl esters 10.1055/S-0028-1084766

Novel potential antitumor analogues of fagaronine and nitidine in the Benzo[c]phenanthroline series 10.1055/S-0028-1084765

Structure-activity relationships in the acronycine and benzo[b]acronycine series: Role of the pyran ring 10.1055/S-0028-1084761

Synthesis and biological evaluation of new disubstituted analogues of 6-methoxy-3-(3 ',4 ',5 '-trimethoxybenzoyl)-1H-indole (BPR0L075), as potential antivascular agents 10.1016/J.BMC.2008.06.002

Synthesis, Cytotoxic Activity, and Mechanism of Action of Furo[2,3-c]acridin-6-one and Benzo[b]furo[3,2-h]acridin-6-one Analogues of Psorospermin and Acronycine 10.1021/JM8009487

A new synthetic access to furo[3,2-f]chromene analogues of an antimycobacterial 10.1016/J.BMC.2008.06.057

Structure-activity relationships in the acronycine and benzo[b]acronycine series: Role of the pyran ring 10.1016/J.EJMECH.2008.01.033

Synthesis, Cytotoxic Activity, and Mechanism of Action of Furo[2,3-c]acridin-6-one and Benzo[b]furo[3,2-h]acridin-6-one Analogues of Psorospermin and Acronycine (vol 51, pg 7287, 2008) 10.1021/JM801396Z

Antitumor Psoropermum Xanthones and Sarcomelicope Acridones: Privileged Structures Implied in DNA Alkylation 10.1021/NP800644Y

Synthesis, cytotoxic activity, and DNA binding properties of antitumor cis-1,2-dihydroxy-1,2-dihydrobenzo[b]acronycine cinnamoyl esters 10.1016/J.BMC.2009.01.062

Diversity-oriented synthesis of furo[3,2-f]chromanes with antimycobacterial activity 10.1016/J.EJMECH.2009.01.017

Cytotoxic activity of Brazilian Cerrado plants used in traditional medicine against cancer cell lines 10.1016/J.JEP.2009.03.018

Acronycine Derivatives: A Promising Series of Anti-Cancer Agents 10.2174/187152009789056921

Isolation and chemistry of the alkaloids from Papaver arachnoideum Kadereit 10.1016/J.BSE.2009.06.007

Synthesis of N-substituted benzo[c][1,7]- and benzo[c][1,8] phenanthrolin-(5H)-6-ones through a Pd-mediated Suzuki-Miyaura heteroaryl-aryl coupling reaction 10.1016/J.TET.2009.09.110

Influence of the Stereoisomeric Position of the Reactive Acetate Groups of the Benzo[b]Acronycine derivative S23906-1 on Its DNA Alkylation, Helix-Opening, Cytotoxic, and Antitumor Activities 10.1124/MOL.109.057554

Tri-ionizable calix[4]arene ligands: synthesis and lanthanide ion complexation 10.3998/ARK.5550190.0011.715

Selective Unusual Pd-Mediated Biaryl Coupling Reactions: Solvent Effects with Carbonate Bases 10.1021/OL902570S

The synthesis and Angiotensin Converting Enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives 10.1016/J.BMCL.2010.01.113

Synthesis and cytotoxic activity of psorospermin and acronycine analogues in the 3-propyloxy-acridin-9(10H)-one and -benzo[b]acridin-12(5H)-one series 10.1016/J.EJMECH.2009.10.045

Synthesis and biological evaluation of dialkylaminoalkylamino benzo[c][1,7] and [1,8]phenanthrolines as antiproliferative agents 10.1016/J.EJMECH.2010.02.043

Structure-activity relationships of indole compounds derived from combretastatin A4: Synthesis and biological screening of 5-phenylpyrrolo[3,4-a]carbazole-1,3-diones as potential antivascular agents 10.1016/J.EJMECH.2010.05.022

Synthesis, biological activity, and evaluation of the mode of action of novel antitubercular benzofurobenzopyrans substituted on A ring 10.1016/J.EJMECH.2010.09.048

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Dammarane Triterpenes from Gardenia aubryi VIEILL 10.1002/HLCA.201000286

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Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents 10.1016/J.EJMECH.2011.02.065

Biological Potential and Structure-Activity Relationships of Most Recently Developed Vascular Disrupting Agents: An Overview of New Derivatives of Natural Combretastatin A-4 10.2174/092986711796391642

Troger's bases in the acronycine, benzo[a]acronycine, and benzo[b]acronycine series 10.1016/J.TETLET.2011.06.064

Solvent/Base Effects in the Selective Domino Synthesis of Phenanthridinones That Involves High-Valent Palladium Species: Experimental and Theoretical Studies 10.1002/CHEM.201101354

Synthesis and Antimicrobial Activities of Some Sulphur Containing Chromene Derivatives 10.1177/1934578X1200700722

A new phenylpropanoid ester from the bark of Zanthoxylum scandens (Rutaceae) 10.1515/ZNC-2002-11-1205

Methodology for the preparation of olive oil open ring secoiridoids 10.1055/S-0032-1321328

New 3,4-secocycloartane and lupane triterpenes from the leaves of the tropical rain forest tree Hopea odorata Roxb 10.1055/S-0032-1321090

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Semisythesis of Guttiferone A analogs 10.1055/S-0032-1320371

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Priscille Brodin

Brodin Priscille

ORCID: 0000-0003-0991-7344

Email: priscille.brodin@inserm.fr

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Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis 10.1126/science.1171583

High Content Screening Identifies Decaprenyl-Phosphoribose 2 ' Epimerase as a Target for Intracellular Antimycobacterial Inhibitors 10.1371/journal.ppat.1000645

Systematic Genetic Nomenclature for Type VII Secretion Systems 10.1371/journal.ppat.1000507

Control of M-tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP 10.1371/journal.ppat.0040033

Aquatic insects and transmission of Mycobacterium ulcerans 10.1051/medsci/20072367572

ESAT-6 from Mycobacterium tuberculosis dissociates from its putative chaperone CFP-10 under acidic conditions and exhibits membrane-lysing activity 10.1128/jb.00469-07

Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis 10.1371/journal.ppat.0030062

Protection against mycobacterium ulcerans lesion development by exposure to aquatic insect saliva 10.1371/journal.pmed.0040064

Support vector machines for automatic detection of tuberculosis bacteria in confocal microscopy images 10.1109/isbi.2007.356794

Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues 10.1016/j.bmc.2006.12.009

An increase in antimycobacterial Th1-cell responses by prime-boost protocols of immunization does not enhance protection against tuberculosis 10.1128/iai.74.4.2128-2137.2006

Benzofuro 3,2-f 1 benzopyrans: A new class of antitubercular agents 10.1016/j.bmc.2006.03.033

Dissection of ESAT-6 system 1 of Mycobacterium tuberculosis and impact on immunogenicity and virulence 10.1128/iai.74.1.88-98.2006

High frequency of CD4(+) T cells specific for the TB10.4 protein correlates with protection against Mycobacterium tuberculosis infection 10.1128/iai.02086-05

Inactivation of Rv2525c, a substrate of the twin arginine translocation (Tat) system of Mycobacterium tuberculosis, increases beta-lactam susceptibility and virulence 10.1128/jb.00631-06

Evaluation of vaccines in the EU TB vaccine cluster using a guinea pig aerosol infection model of tuberculosis 10.1016/j.tube.2004.09.009

Functional analysis of early secreted antigenic target-6, the dominant T-cell antigen of Mycobacterium tuberculosis, reveals key residues involved in secretion, complex formation, virulence, and immunogenicity 10.1074/jbc.M503515200

Immunogenic membrane-associated proteins of Mycobacterium tuberculosis revealed by proteomics 10.1099/mic.0.27799-0

Proteomic identification of M. tuberculosis protein kinase substrates: PknB recruits GarA, a FHA domain-containing protein, through activation loop-mediated interactions 10.1016/j.jmb.2005.05.049

Tuberculosis: from genome to vaccine 10.1586/14760584.4.4.541

Cell envelope protein PPE68 contributes to Mycobacterium tuberculosis RDI immunogenicity independently of a 10-kilodalton culture filtrate protein and ESAT-6 10.1128/iai.72.4.2170-2176.2004

Enhanced protection against tuberculosis by vaccination with recombinant Mycobacterium microti vaccine that induces T cell immunity against region of difference 1 antigens 10.1086/421468

ESAT-6 proteins: protective antigens and virulence factors? 10.1016/j.tim.2004.09.007

Macro-array and bioinformatic analyses reveal mycobacterial 'core' genes, variation in the ESAT-6 gene family and new phylogenetic markers for the Mycobacterium tuberculosis complex 10.1099/mic.0.26662-0

CD8(+)-T-cell responses of mycobacterium-infected mice to a newly identified major histocompatibility complex class I-restricted epitope shared by proteins of the ESAT-6 family 10.1128/iai.71.12.7173-7177.2003

Recombinant BCG exporting ESAT-6 confers enhanced protection against tuberculosis 10.1038/nm859

A new evolutionary scenario for the Mycobacterium tuberculosis complex 10.1073/pnas.052548299

Bacterial artificial chromosome-based comparative genomic analysis identifies Mycobacterium microti as a natural ESAT-6 deletion mutant 10.1128/iai.70.10.5568-5578.2002

Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides 10.1021/bi015732y

Loss of RD1 contributed to the attenuation of the live tuberculosis vaccines Mycobacterium bovis BCG and Mycobacterium microti 10.1046/j.1365-2958.2002.03237.x

6-Oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro 10.1081/ncn-100002322

Determinants of Mg2+-dependent activities of recombinant human immunodeficiency virus type 1 integrase 10.1021/bi000398b

Inhibition of the human immunodeficiency virus type 1 DNA integration by modified oligonucleotides 10.1023/a:1026631910681

Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase 10.1016/s0014-5793(99)01350-2

Inhibition of HIV-1 integration by mono- & bi-functionalized triple helix forming oligonucleotides 10.1080/07328319908044831

Optimization of alternate-strand triple helix formation at the 5 '-TpA-3 ' and 5 '-ApT-3 ' junctions 10.1093/nar/27.15.3029

A truncated HIV-1 Tat protein basic domain rapidly translocates through the plasma membrane and accumulates in the cell nucleus 10.1074/jbc.272.25.16010

Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371 10.15252/embr.201744371.

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles 10.1038/s41598-017-05453-3

Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4 10.1038/s41598-017-11843-4.

Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays 10.1021/acschembio.7b00091

Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017 10.1016/j.mib.2017.11.017.

Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020 10.1016/j.chom.2017.07.020. Epub 2017 Aug 31.

Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101 10.1016/j.celrep.2017.08.101.

Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114 10.1073/pnas.1707840114.

Identification of Piperazinylbenzenesulfonamides as New Inhibitors of Claudin-1 Trafficking and Hepatitis C Virus Entry 10.1128/jvi.01982-17

Multiplexed Quantitation of Intraphagocyte Mycobacterium tuberculosis Secreted Protein Effectors 10.1016/j.celrep.2018.03.125

Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis 10.1016/j.bioorg.2018.08.025

Proteomics of Mycobacterium infection: Moving towards a Better Understanding of Pathogen-Driven immunomodulation 10.3389/fimmu.2018.00086

Synergy between circular bacteriocin AS-48 and ethambutol against Mycobacterium tuberculosis 10.1128/aac.00359-18

The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase 10.1016/j.tube.2018.08.004

Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4

Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs 10.1016/j.ijpharm.2017.05.030

Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017

Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020

Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101

Phenotypic assays for Mycobacterium tuberculosis infection 10.1002/cyto.a.23129

A fast, fully automated cell segmentation algorithm for high-throughput and high-content screening 10.1002/cyto.a.20627

Compartmentalized Encapsulation of Two Antibiotics in Porous Nanoparticles: an Efficient Strategy to Treat Intracellular Infections 10.1002/ppsc.201800360

Spatiotemporal Changes of the Phagosomal Proteome in Dendritic Cells in Response to LPS Stimulation 10.1074/mcp.RA119.001316

Mycolactone as Analgesic: Subcutaneous Bioavailability Parameters 10.3389/fphar.2019.00378

Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis 10.1021/acsnano.8b07902

Mitochondrial Dynamics and Activity in Legionella-Infected Cells 10.1007/978-1-4939-9048-1_13

Heparin-Binding Hemagglutinin Adhesin (HBHA) Is Involved in Intracytosolic Lipid Inclusions Formation in Mycobacteria 10.3389/fmicb.2018.02258

Dehydrojuncusol, a Natural Phenanthrene Compound Extracted from Juncus maritimus, Is a New Inhibitor of Hepatitis C Virus RNA Replication 10.1128/jvi.02009-18

A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation 10.1039/C9OB00680J

Could Mycolactone Inspire New Potent Analgesics? Perspectives and Pitfalls 10.3390/toxins11090516

Paradoxical Roles of the MAL/Tirap Adaptor in Pathologies. 10.3389/fimmu.2020.569127

Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity. 10.1021/acsinfecdis.9b00277

Intracellular and in vivo evaluation of imidazo[2,1-b]thiazole-5-carboxamide anti-tuberculosis compounds. 10.1371/journal.pone.0227224

Preclinical assessment of a new live attenuated Mycobacterium tuberculosis Beijing-based vaccine for tuberculosis. 10.1016/j.vaccine.2019.11.085

IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection 10.1101/761551

Worms' Antimicrobial Peptides. 10.3390/md17090512

T(oo)bAd. 10.1038/s41589-019-0347-x

Theaflavins, polyphenols of black tea, inhibit entry of hepatitis C virus in cell culture. 10.1371/journal.pone.0198226

Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro. 10.3389/fmicb.2015.00488

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. 10.1038/nm.3262

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g

Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease. 10.1186/1753-6561-5-s1-p38

Automated HTS/HCS for antivirals using visual HIV full replication assays. 10.1186/1742-4690-6-s2-p82

Influence of ESAT-6 secretion system 1 (RD1) of Mycobacterium tuberculosis on the interaction between mycobacteria and the host immune system. 10.4049/jimmunol.174.6.3570

Cell microbiology interview 10.1111/cmi.13288

Pathogenomic analyses of Mycobacterium microti, an ESX-1-deleted member of the Mycobacterium tuberculosis complex causing disease in various hosts 10.1099/mgen.0.000505

Nathalie deboosere

deboosere Nathalie

ORCID: 0000-0002-2873-5485

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton. 10.15252/embr.201744371

Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling. 10.1016/j.celrep.2017.08.101

A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone. 10.3390/toxins9070227

Phenotypic assays for Mycobacterium tuberculosis infection. 10.1002/cyto.a.23129

Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays. 10.1021/acschembio.7b00091

STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection. 10.1038/srep29297

LppM impact on the colonization of macrophages by Mycobacterium tuberculosis. 10.1111/cmi.12619

A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening. 10.3791/51114

Adhesion of human pathogenic enteric viruses and surrogate viruses to inert and vegetal food surfaces. 10.1016/j.fm.2012.04.007

Viral elution and concentration method for detection of influenza A viruses in mud by real-time RT-PCR. 10.1016/j.jviromet.2011.10.013

Comparison of chlorine and peroxyacetic-based disinfectant to inactivate Feline calicivirus, Murine norovirus and Hepatitis A virus on lettuce. 10.1016/j.ijfoodmicro.2011.08.011

Direct detection of highly pathogenic avian influenza A/H5N1 virus from mud specimens. 10.1016/j.jviromet.2011.06.002

Development and validation of a concentration method for the detection of influenza a viruses from large volumes of surface water. 10.1128/aem.02484-10

A predictive microbiology approach for thermal inactivation of Hepatitis A virus in acidified berries. 10.1016/j.fm.2010.05.018

Assessment of the removal and inactivation of influenza viruses H5N1 and H1N1 by drinking water treatment. 10.1016/j.watres.2010.01.013

Intra-laboratory validation of a concentration method adapted for the enumeration of infectious F-specific RNA coliphage, enterovirus, and hepatitis A virus from inoculated leaves of salad vegetables. 10.1016/j.ijfoodmicro.2005.11.007

Modelling effect of physical and chemical parameters on heat inactivation kinetics of hepatitis A virus in a fruit model system. 10.1016/j.ijfoodmicro.2003.10.015

Host-pathogen systems for early drug discovery against tuberculosis. 10.1016/j.mib.2017.11.017

Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids. 10.1073/pnas.1707840114

Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis. 10.1038/s41598-017-11843-4

Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages. 10.1016/j.chom.2017.07.020

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-017-05453-3

Host-directed therapies offer novel opportunities for the fight against tuberculosis. 10.1016/j.drudis.2017.05.005

Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs. 10.1016/j.ijpharm.2017.05.030

Impact of pe_pgrs33 Gene Polymorphisms on Mycobacterium tuberculosis Infection and Pathogenesis. 10.3389/fcimb.2017.00137

Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections. 10.2217/nnm-2016-0364

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. 10.1126/science.aag1006

How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011

Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism. 10.1007/s00401-016-1652-z

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535

Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization. 10.1016/j.str.2016.07.009

Khaya grandifoliola C.DC: a potential source of active ingredients against hepatitis C virus in vitro. 10.1007/s00705-016-2771-5

[Mycolactone: the amazing analgesic mycobacterial toxin]. 10.1051/medsci/20163202007

A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. 10.1039/c5ob02630j

Polyphenols Inhibit Hepatitis C Virus Entry by a New Mechanism of Action. 10.1128/jvi.01473-15

Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro. 10.3389/fmicb.2015.00488

Increased protective efficacy of recombinant BCG strains expressing virulence-neutral proteins of the ESX-1 secretion system. 10.1016/j.vaccine.2015.03.083

Cytosolic access of Mycobacterium tuberculosis: critical impact of phagosomal acidification control and demonstration of occurrence in vivo. 10.1371/journal.ppat.1004650

[High content screening in chemical biology: overview and main challenges]. 10.1051/medsci/20153102016

Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. 10.1007/978-1-4939-2450-9_24

2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1. 10.1021/cb5007163

High-content screening technology combined with a human granuloma model as a new approach to evaluate the activities of drugs against Mycobacterium tuberculosis. 10.1128/aac.03705-14

Mycobacterial toxin induces analgesia in buruli ulcer by targeting the angiotensin pathways. 10.1016/j.cell.2014.04.040

Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches. 10.1021/jm500422b

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. 10.1038/nm.3262

The balance of apoptotic and necrotic cell death in Mycobacterium tuberculosis infected macrophages is not dependent on bacterial virulence. 10.1371/journal.pone.0047573

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g

Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200825u

A novel specific edge effect correction method for RNA interference screenings. 10.1093/bioinformatics/btr648

Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis. 10.1371/journal.pone.0026675

High-content screening in infectious diseases. 10.1016/j.cbpa.2011.05.023

Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200076a

Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease. 10.1186/1753-6561-5-s1-p38

High content phenotypic cell-based visual screen identifies Mycobacterium tuberculosis acyltrehalose-containing glycolipids involved in phagosome remodeling. 10.1371/journal.ppat.1001100

High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery. 10.4155/fmc.10.223

Functional characterization of the Mycobacterium tuberculosis serine/threonine kinase PknJ. 10.1099/mic.0.038133-0

High content screening identifies decaprenyl-phosphoribose 2' epimerase as a target for intracellular antimycobacterial inhibitors. 10.1371/journal.ppat.1000645

Systematic genetic nomenclature for type VII secretion systems. 10.1371/journal.ppat.1000507

Long-circulating DNA lipid nanocapsules as new vector for passive tumor targeting. 10.1016/j.biomaterials.2009.09.044

Automated HTS/HCS for antivirals using visual HIV full replication assays. 10.1186/1742-4690-6-s2-p82

Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. 10.1126/science.1171583

Automated high-throughput siRNA transfection in raw 264.7 macrophages: a case study for optimization procedure. 10.1177/1087057108328762

Control of M. tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP. 10.1371/journal.ppat.0040033

ESAT-6 from Mycobacterium tuberculosis dissociates from its putative chaperone CFP-10 under acidic conditions and exhibits membrane-lysing activity. 10.1128/jb.00469-07

[Aquatic insects and transmission of Mycobacterium ulcerans]. 10.1051/medsci/20072367572

Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis. 10.1371/journal.ppat.0030062

Protection against Mycobacterium ulcerans lesion development by exposure to aquatic insect saliva. 10.1371/journal.pmed.0040064

Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues. 10.1016/j.bmc.2006.12.009

Inactivation of Rv2525c, a substrate of the twin arginine translocation (Tat) system of Mycobacterium tuberculosis, increases beta-lactam susceptibility and virulence. 10.1128/jb.00631-06

High frequency of CD4+ T cells specific for the TB10.4 protein correlates with protection against Mycobacterium tuberculosis infection. 10.1128/iai.02086-05

Benzofuro[3,2-f][1]benzopyrans: a new class of antitubercular agents. 10.1016/j.bmc.2006.03.033

An increase in antimycobacterial Th1-cell responses by prime-boost protocols of immunization does not enhance protection against tuberculosis. 10.1128/iai.74.4.2128-2137.2006

Dissection of ESAT-6 system 1 of Mycobacterium tuberculosis and impact on immunogenicity and virulence. 10.1128/iai.74.1.88-98.2006

Tuberculosis: from genome to vaccine. 10.1586/14760584.4.4.541

Immunogenic membrane-associated proteins of Mycobacterium tuberculosis revealed by proteomics. 10.1099/mic.0.27799-0

Influence of ESAT-6 secretion system 1 (RD1) of Mycobacterium tuberculosis on the interaction between mycobacteria and the host immune system. 10.4049/jimmunol.174.6.3570

Evaluation of vaccines in the EU TB Vaccine Cluster using a guinea pig aerosol infection model of tuberculosis. 10.1016/j.tube.2004.09.009

ESAT-6 proteins: protective antigens and virulence factors? 10.1016/j.tim.2004.09.007

Enhanced protection against tuberculosis by vaccination with recombinant Mycobacterium microti vaccine that induces T cell immunity against region of difference 1 antigens. 10.1086/421468

Cell envelope protein PPE68 contributes to Mycobacterium tuberculosis RD1 immunogenicity independently of a 10-kilodalton culture filtrate protein and ESAT-6. 10.1128/iai.72.4.2170-2176.2004

CD8+-T-cell responses of Mycobacterium-infected mice to a newly identified major histocompatibility complex class I-restricted epitope shared by proteins of the ESAT-6 family. 10.1128/iai.71.12.7173-7177.2003

Recombinant BCG exporting ESAT-6 confers enhanced protection against tuberculosis. 10.1038/nm859

Loss of RD1 contributed to the attenuation of the live tuberculosis vaccines Mycobacterium bovis BCG and Mycobacterium microti. 10.1046/j.1365-2958.2002.03237.x

Bacterial artificial chromosome-based comparative genomic analysis identifies Mycobacterium microti as a natural ESAT-6 deletion mutant. 10.1128/iai.70.10.5568-5578.2002

Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides. 10.1021/bi015732y

IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection 10.1101/761551

Large scale screening discovers clofoctol as an inhibitor of SARS-CoV-2 replication that reduces COVID-19-like pathology 10.1101/2021.06.30.450483

Yves Janin

Janin Yves / Yves L. Janin

ORCID: 0000-0003-3019-9842

A Bioluminescent 3CLPro Activity Assay to Monitor SARS-CoV-2 Replication and Identify Inhibitors 10.3390/v13091814

A Study of Negishi Cross-Coupling Reactions with Benzylzinc Halides To Prepare Original 3-Ethoxypyrazoles 10.1055/s-0034-1379458

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH). 10.1021/acs.jmedchem.5b00606

Original 2-(3-Alkoxy-1H-pyrazol-1-yl)pyrimidine Derivatives as Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH). 10.1021/jm501446r

Bioassay-Guided Fractionation of Extracts from Codiaeum variegatum against Entamoeba histolytica Discovers Compounds That Modify Expression of Ceramide Biosynthesis Related Genes 10.1371/journal.pntd.0002607

Non-quinolone Inhibitors of Bacterial Type IIA Topoisomerases: A Feat of Bioisosterism 10.1021/cr4003984

On Dihydroorotate Dehydrogenases and Their Inhibitors and Uses 10.1021/jm301848w

Preparations of 4-Substituted 3-Carboxypyrazoles 10.1002/jhet.1654

Pyrazole-3/5-carboxylic acids from 3/5-trifluoromethyl NH-pyrazoles 10.1016/j.tet.2012.10.034

3-Methoxypyrazoles from 1,1-dimethoxyethene, few original results 10.1016/j.tet.2012.02.057

Few unexpected results from a Suzuki-Miyaura reaction 10.1016/j.tet.2012.01.019

Preparation and Chemistry of 3/5-Halogenopyrazoles 10.1021/cr200427q

On the Knorr Synthesis of 6-Bromo-4-methylquinolin-2(1H)-one 10.1055/s-0030-1258440

Simple preparations of 4 and 5-iodinated pyrazoles as useful building blocks 10.1016/j.tet.2011.09.029

5-Iodo-3-Ethoxypyrazoles: An Entry Point to New Chemical Entities 10.1002/chem.200903442

ATPase inhibitors of heat-shock protein 90 second season 10.1016/j.drudis.2010.03.002

N-arylation of 3-alkoxypyrazoles, the case of the pyridines 10.1016/j.tet.2010.02.032

Synthesis, biological activity, and evaluation of the mode of action of novel antitubercular benzofurobenzopyrans substituted on A ring 10.1016/j.ejmech.2010.09.048

4-Arylation of 3-alkoxypyrazoles 10.1016/j.tet.2009.01.109

Diversity-oriented synthesis of furo 3,2-f chromanes with antimycobacterial activity 10.1016/j.ejmech.2009.01.017

Nitrogen's reactivity of various 3-alkoxypyrazoles 10.1016/j.tet.2009.01.099

A new synthetic access to furo 3,2-f chromene analogues of an antimycobacterial 10.1016/j.bmc.2008.06.057

An Improved Preparation of 3-Alkoxypyrazoles 10.1055/s-0028-1083186

Antimycobacterial benzofuro 3,2-f chromenes from a 5-bromochromen-6-ol 10.1055/s-2007-966019

Antituberculosis drugs: Ten years of research 10.1016/j.bmc.2007.01.030

Isoxyl activation is required for bacteriostatic activity against Mycobacterium tuberculosis 10.1128/aac.00433-07

Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues 10.1016/j.bmc.2006.12.009

Heat shock protein 90 inhibitors. A text book example of medicinal chemistry? 10.1021/jm050759r

Synthesis of methylenedioxy-bearing 1-aryl-3-carboxylisoquinolines using a modified Ritter reaction procedure 10.1016/j.tet.2004.05.004

Peptides with anticancer use or potential 10.1007/s00726-002-0349-x

2-amino-3-(3-hydroxy-1,2,5-thiadiazol-4-yl)propionic acid: Resolution, absolute stereochemistry and enantiopharmacology at glutamate receptors 10.1016/s0968-0896(02)00041-x

Synthesis of chloramphenicol and mandelonitrile galactose-containing prodrugs 10.1081/car-120013493

Synthetic approaches to 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid 10.1039/b110301f

3-Pyrazolone analogues of the 3-isoxazolol metabotropic excitatory amino acid receptor agonist homo-AMPA. Synthesis and pharmacological testing 10.1016/s0223-5234(99)00122-1

On the methylation of 3-cyano-6-hydroxypyridine-2(1H)-ones 10.1016/s0040-4020(99)00755-3

Rational design of a triple helix-specific intercalating ligand 10.1073/pnas.95.7.3591

Unambiguous synthesis of 1-methyl-3-hydroxypyrazoles 10.1016/s0040-4020(98)00579-1

1,3-dipolar cycloaddition approach to the construction of new bis- heterocycles from thymine as potential non-nucleoside reverse transcriptase inhibitors 10.1039/a605995c

Imidazo 1,5-g 1,4 diazepines, TIBO analogues lacking the phenyl ring: Synthesis and evaluation as anti-HIV agents 10.1016/s0040-4020(96)00952-0

Isoxazoles as latent alpha-cyanoaldehydes: Construction of the indole 2,3-a quinolizine ring system 10.1016/0040-4020(95)00931-0

A FORMAL NEW ACCESS TO THE BENZO C PHENANTHRIDINE ALKALOIDS, SYNTHESIS OF NITIDINE AND O-METHYL FAGARONINE ANALOGS 10.1016/s0040-4020(01)80559-7

SYNTHESIS AND EVALUATION OF NEW 6-AMINO-SUBSTITUTED BENZO C PHENANTHRIDINE DERIVATIVES 10.1021/jm00075a025

Respiratory syncytial virus infection in macaques is not suppressed by intranasal sprays of pyrimidine biosynthesis inhibitors. 10.1016/j.antiviral.2015.11.006

1 Synthetic Routes to Coelenterazine and Other Imidazo[1,2-a]pyrazin-3-one Luciferins: Essential Tools for Bioluminescence-Based Investigations 10.1002/chem.201501531

Synthesis and evaluation of original bioisosteres of bacterial type IIA topoisomerases inhibitors 10.1139/cjc-2015-0475

Checkpoint kinase 1 inhibition sensitises transformed cells to dihydroorotate dehydrogenase inhibition. 10.18632/oncotarget.19199

Synthesis of alpha-Amino Esters via alpha-Nitro or alpha-Oxime Esters: A Review 10.1055/s-0036-1589506

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