Portrait

Prof. Dr.

Marc Nazaré

Head Nazaré Group

 +49 30 94793 581

+49 30 94063 084

 nazare@fmp-berlin.de

0000-0002-1602-2330

Marc Nazare studied chemistry at the University of Karlsruhe and obtained his PhD in organic chemistry with Herbert Waldmann in the field of natural product total synthesis in 1999. He then joined pharmaceutical industry at Sanofi in Frankfurt as a medicinal chemist. In 2013, Dr. Nazaré started a medicinal chemistry group at the Leibniz Research Institute for Molecular Pharmacology FMP. His current research interests are focused on the design and optimization of chemical probes and imaging tools for chemical biology and translational applications. He is a honorary professor at the University Bielefeld.


Chemical Biology


Nazaré Group


FMP
UB

Structure-Based Design of Xanthine-Imidazopyridines and -Imidazothiazoles as Highly Potent and In Vivo Efficacious Tryptophan Hydroxylase Inhibitors.

  • Specker E; Wesolowski R; Schütz A; Matthes S; Mallow K; Wasinska-Kalwa M; Winkler L; Oder A; Alenina N; Pleimes D; von Kries JP; Heinemann U; Bader M; Nazaré M

Journal of medicinal chemistry 2023

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Discovery of tetrazolo-pyridazine-based small molecules as inhibitors of MACC1-driven cancer metastasis.

  • Yan S; Schöpe PC; Lewis J; Putzker K; Uhrig U; Specker E; von Kries JP; Lindemann P; Omran A; Sanchez-Ibarra HE; Unger A; Zischinsky ML; Klebl B; Stein U

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 2023

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Structural Basis for Highly Selective Class II Alpha Phosphoinositide-3-Kinase Inhibition.

  • Kücükdisli M; Bel-Abed H; Cirillo D; Lo WT; Efrém NL; Horatscheck A; Perepelittchenko L; Prokofeva P; Ehret TAL; Radetzki S; Neuenschwander M; Nazaré M

Journal of medicinal chemistry 2023

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Selective and pH-Independent Detection of Ba<sup>2+</sup> in Water by a Benzo-21-crown-7-Functionalized BODIPY.

  • Sprenger T; Schwarze T; Müller H; Sperlich E; Holdt HJ; Nazaré M; Hentsch A; Eidner S; Kraft R; Kumke MU

Chemistry (Weinheim an der Bergstrasse, Germany) 2023

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CLK2 and CLK4 are regulators of DNA damage-induced NF-κB targeted by novel small molecule inhibitors.

  • Mucka P; Lindemann P; Bosco B; Willenbrock M; Radetzki S; Neuenschwander M; Brischetto C; Peter von Kries J; Nazaré M; Scheidereit C

Cell chemical biology 2023

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Aβ Chronic Exposure Promotes an Activation State of Microglia through Endocannabinoid Signalling Imbalance.

  • Scipioni L; Tortolani D; Ciaramellano F; Fanti F; Gazzi T; Sergi M; Nazaré M; Oddi S; Maccarrone M

International journal of molecular sciences 2023

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First <i>in vivo</i> fluorine-19 magnetic resonance imaging of the multiple sclerosis drug siponimod.

  • Starke L; Millward JM; Prinz C; Sherazi F; Waiczies H; Lippert C; Nazaré M; Paul F; Niendorf T; Waiczies S

Theranostics 2023

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Small molecule inhibiting microglial nitric oxide release could become a potential treatment for neuroinflammation.

  • Jordan P; Costa A; Specker E; Popp O; Volkamer A; Piske R; Obrusnik T; Kleissle S; Stuke K; Rex A; Neuenschwander M; von Kries JP; Nazare M; Wolf SA

PloS one 2023

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Isoform-selective targeting of PI3K: time to consider new opportunities?

  • Davide Cirillo; Marta Diceglie; Marc Nazaré

Trends in Pharmacological Sciences 2023

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CB2R agonists in the clinics: A treasure chest for treating inflammatory diseases

  • Uwe Grether; Marc Nazaré

Open Access Government 2023

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CB₂R ligands to treat inflammatory diabetes

  • Uwe Grether; Marc Nazaré

Open Access Government 2023

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Phosphoinositide Conversion Inactivates R-RAS and Drives Metastases in Breast Cancer.

  • Li H; Prever L; Hsu MY; Lo WT; Margaria JP; De Santis MC; Zanini C; Forni M; Novelli F; Pece S; Di Fiore PP; Porporato PE; Martini M; Belabed H; Hirsch E

Advanced science (Weinheim, Baden-Wurttemberg, Germany) 2022

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Probing Factor Xa Protein-Ligand Interactions: Accurate Free Energy Calculations and Experimental Validations of Two Series of High-Affinity Ligands.

  • Fernández-Bachiller MI; Hwang S; Schembri ME; Lindemann P; Guberman M; Herziger S; Specker E; Matter H; Will DW; Czech J; Wagner M; Bauer A; Nazaré M

Journal of medicinal chemistry 2022

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Identification of the Allosteric Binding Site for Thiazolopyrimidine on the C-Type Lectin Langerin.

  • Zhang H; Modenutti C; Nekkanti YPK; Denis M; Bermejo IA; Lefèbre J; Che K; Kim D; Kagelmacher M; Kurzbach D; Nazaré M; Rademacher C

ACS chemical biology 2022

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Development of selective inhibitors of phosphatidylinositol 3-kinase C2α.

  • Lo WT; Belabed H; Kücükdisli M; Metag J; Roske Y; Prokofeva P; Ohashi Y; Horatscheck A; Cirillo D; Krauss M; Schmied C; Neuenschwander M; Haucke V

Nature chemical biology 2022

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Structure-Based Design of Xanthine-Benzimidazole Derivatives as Novel and Potent Tryptophan Hydroxylase Inhibitors.

  • Specker E; Matthes S; Wesolowski R; Schütz A; Grohmann M; Alenina N; Pleimes D; Mallow K; Neuenschwander M; Gogolin A; Weise M; Pfeifer J; Ziebart N; Bader M

Journal of medicinal chemistry 2022

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An LPAR <sub><b>5</b></sub> -antagonist that reduces nociception and increases pruriception.

  • Langedijk J; Araya EI; Barroso AR; Tolenaars D; Nazaré M; Belabed H; Schoene J; Chichorro JG; Oude Elferink R

Frontiers in pain research (Lausanne, Switzerland) 2022

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Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe.

  • Gazzi T; Brennecke B; Atz K; Korn C; Sykes D; Forn-Cuni G; Pfaff P; Sarott RC; Westphal MV; Mostinski Y; Mach L; Wasinska-Kalwa M; Weise M; Hoare BL; Nazaré M

Chemical science 2022

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Rational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis

  • Nis Halland; Friedemann Schmidt; Tilo Weiss; Ziyu Li; Jörg Czech; Joachim Saas; Danping Ding-Pfennigdorff; Matthias K. Dreyer; Carsten Strübing; Marc Nazare

Journal of Medicinal Chemistry 2022

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Donor manipulation for constructing a pH sensing thermally activated delayed fluorescent probe to detect alkaliphiles

  • Qian Liu; Miao Yang; Xiangchuan Meng; Xiaowan Han; Marc Nazare; Youjun Xu; Hai-Yu Hu; Qingyang Zhang

Talanta 2022

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Antagonistic control of active surface integrins by myotubularin and phosphatidylinositol 3-kinase C2β in a myotubular myopathy model

  • Paula Samsó; Philipp A. Koch; York Posor; Wen-Ting Lo; Hassane Belabed; Marc Nazare; Jocelyn Laporte; Volker Haucke

Proceedings of the National Academy of Sciences 2022

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Reverse-Design toward Optimized Labeled Chemical Probes – Examples from the Endocannabinoid System

  • Mónica Guberman; Miroslav Kosar; Anahid Omran; Erick M. Carreira; Marc Nazaré; Uwe Grether

CHIMIA 2022

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Compound Interaction Screen on a Photoactivatable Cellulose Membrane (CISCM) Identifies Drug Targets

  • F. Teresa I. Melder; Peter Lindemann; Alexander Welle; Vanessa Trouillet; Stefan Heißler; Marc Nazaré; Matthias Selbach

ChemMedChem 2022

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Weizhouochrones: Gorgonian-Derived Symmetric Dimers and Their Structure Elucidation Using Anisotropic NMR Combined with DP4+ Probability and CASE-3D

  • Xiao-Lu Li; Tong Ru; Armando Navarro-Vázquez; Peter Lindemann; Marc Nazaré; Xu-Wen Li; Yue-Wei Guo; Han Sun

Journal of Natural Products 2022

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Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II.

  • Leenders RGG; Brinch SA; Sowa ST; Amundsen-Isaksen E; Galera-Prat A; Murthy S; Aertssen S; Smits JN; Nieczypor P; Damen E; Wegert A; Nazaré M; Krauss S

Journal of medicinal chemistry 2021

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Topical inflammasome inhibition with disulfiram prevents irritant contact dermatitis.

  • Bonnekoh H; Vera C; Abad-Perez A; Radetzki S; Neuenschwander M; Specker E; Mahnke NA; Frischbutter S; Latz E; Nazaré M; Kries JV; Maurer M; Scheffel J; Krause K

Clinical and translational allergy 2021

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Functional Imaging Using Fluorine (<sup>19</sup>F) MR Methods: Basic Concepts.

  • Waiczies S; Prinz C; Starke L; Millward JM; Delgado PR; Rosenberg J; Nazaré M; Waiczies H; Pohlmann A; Niendorf T

Methods in molecular biology (Clifton, N.J.) 2021

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<i>In vivo</i> detection of teriflunomide-derived fluorine signal during neuroinflammation using fluorine MR spectroscopy.

  • Prinz C; Starke L; Millward JM; Fillmer A; Delgado PR; Waiczies H; Pohlmann A; Rothe M; Nazaré M; Paul F; Niendorf T; Waiczies S

Theranostics 2021

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DOTAM-Based, Targeted, Activatable Fluorescent Probes for the Highly Sensitive and Selective Detection of Cancer Cells

  • Benjamin Brennecke; Qinghua Wang; Wolfgang Haap; Uwe Grether; Hai-Yu Hu; Marc Nazaré

Bioconjugate Chemistry 2021

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Enhanced Properties of a Benzimidazole Benzylpyrazole Lysine Demethylase Inhibitor: Mechanism-of-Action, Binding Site Analysis, and Activity in Cellular Models of Prostate Cancer

  • David M. Carter; Edgar Specker; Piotr H. Małecki; Jessica Przygodda; Krystyna Dudaniec; Manfred S. Weiss; Udo Heinemann; Marc Nazaré; Ulrich Gohlke

Journal of Medicinal Chemistry 2021

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Pentafluorosulfanyl (SF<sub>5</sub>) as a Superior <sup>19</sup>F Magnetic Resonance Reporter Group: Signal Detection and Biological Activity of Teriflunomide Derivatives.

  • Prinz C; Starke L; Ramspoth TF; Kerkering J; Martos Riaño V; Paul J; Neuenschwander M; Oder A; Radetzki S; Adelhoefer S; Ramos Delgado P; Aravina M; Waiczies S

ACS sensors 2021

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Cannabinoid receptor type 2 ligands: an analysis of granted patents since 2010

  • Benjamin Brennecke; Thais Gazzi; Kenneth Atz; Jürgen Fingerle; Pascal Kuner; Torsten Schindler; Guy de Weck; Marc Nazaré; Uwe Grether

Pharmaceutical Patent Analyst 2021

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Diverse chemotypes drive biased signaling by cannabinoid receptors

  • Miljuš T; Heydenreich FM; Gazzi T; Kimbara A; Rogers-Evans M; Nettekoven M; Zirwes E; Osterwald A; Rufer AC; Ullmer C; Guba W; Le Gouill C; Veprintsev DB
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Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells.

  • Sarott RC; Westphal MV; Pfaff P; Korn C; Sykes DA; Gazzi T; Brennecke B; Atz K; Weise M; Mostinski Y; Hompluem P; Koers E; Miljuš T; Roth NJ; Carreira EM

Journal of the American Chemical Society 2020

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Revealing cytotoxic substructures in molecules using deep learning

  • Henry E. Webel; Talia B. Kimber; Silke Radetzki; Martin Neuenschwander; Marc Nazaré; Andrea Volkamer

Journal of Computer-Aided Molecular Design 2020

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Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie 2020

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An Activatable Lanthanide Luminescent Probe for Time‐Gated Detection of Nitroreductase in Live Bacteria

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie International Edition 2020

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Back Cover: An Activatable Lanthanide Luminescent Probe for Time‐Gated Detection of Nitroreductase in Live Bacteria (Angew. Chem. Int. Ed. 22/2020)

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie International Edition 2020

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Rücktitelbild: Eine aktivierbare Lanthanoid‐Lumineszenzsonde für die zeitgesteuerte Detektion von Nitroreduktase in lebenden Bakterien (Angew. Chem. 22/2020)

  • Benjamin Brennecke; Qinghua Wang; Qingyang Zhang; Hai‐Yu Hu; Marc Nazaré

Angewandte Chemie 2020

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Dual-Mode Detection of Bacterial 16S Ribosomal RNA in Tissues

  • Shengnan Xu; Qingyang Zhang; Xiaowan Han; Yali Wang; Xiang Wang; Marc Nazare; Jian-Dong Jiang; Hai-Yu Hu

ACS Sensors 2020

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A Palladium-Catalyzed Domino Reaction To Access 3-Amino-2H-indazoles from Hydrazines and 2-Halobenzonitriles

  • Rana Alsalim; Peter Lindemann; María Pascual López-Alberca; Sandra Miksche; Werngard Czechtizky; Nis Halland; Marc Nazaré

Organic Letters 2020

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Preclinical Lead Optimization of a 1,2,4-Triazole Based Tankyrase Inhibitor.

  • Waaler J; Leenders RGG; Sowa ST; Alam Brinch S; Lycke M; Nieczypor P; Aertssen S; Murthy S; Galera-Prat A; Damen E; Wegert A; Nazaré M; Lehtiö L; Krauss S

Journal of medicinal chemistry 2020

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NMR quality control of fragment libraries for screening.

  • Sreeramulu S; Richter C; Kuehn T; Azzaoui K; Blommers MJJ; Del Conte R; Fragai M; Trieloff N; Schmieder P; Nazaré M; Specker E; Ivanov V; Schwalbe H

Journal of biomolecular NMR 2020

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Designed nanomolar small-molecule inhibitors of Ena/VASP EVH1 interaction impair invasion and extravasation of breast cancer cells.

  • Barone M; Müller M; Chiha S; Ren J; Albat D; Soicke A; Dohmen S; Klein M; Bruns J; van Dinther M; Opitz R; Lindemann P; Beerbaum M; Motzny K; Kühne R

Proceedings of the National Academy of Sciences of the United States of America 2020

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From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.

  • Mostinski Y; Heynen GJJE; López-Alberca MP; Paul J; Miksche S; Radetzki S; Schaller D; Shanina E; Seyffarth C; Kolomeets Y; Ziebart N; de Schryver J; Nazaré M

Journal of medicinal chemistry 2020

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A novel nitroreductase-enhanced MRI contrast agent and its potential application in bacterial imaging

  • Liu, Y.; Zhang, L.; Nazare, M.; Yao, Q.; Hu, H.-Y.

Acta Pharmaceutica Sinica B 2018

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Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase.

  • Ruess DA; Heynen GJ; Ciecielski KJ; Ai J; Berninger A; Kabacaoglu D; Görgülü K; Dantes Z; Wörmann SM; Diakopoulos KN; Karpathaki AF; Kowalska M; Algül H

Nature medicine 2018

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Identification and Characterization of a Single High-Affinity Fatty Acid Binding Site in Human Serum Albumin.

  • Wenskowsky L; Schreuder H; Derdau V; Matter H; Volkmar J; Nazaré M; Opatz T; Petry S

Angewandte Chemie (International ed. in English) 2018

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A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus-Silane System.

  • Schoene J; Bel Abed H; Schmieder P; Christmann M; Nazaré M

Chemistry (Weinheim an der Bergstrasse, Germany) 2018

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Allosteric Inhibition of a Mammalian Lectin

  • Jonas Aretz; Upendra R. Anumala; Felix F. Fuchsberger; Narges Molavi; Nandor Ziebart; Hengxi Zhang; Marc Nazaré; Christoph Rademacher

Journal of the American Chemical Society 2018

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CellFy-A Cell-Based Fragment Screen against C-Type Lectins.

  • Schulze J; Baukmann H; Wawrzinek R; Fuchsberger F; Specker E; Aretz J; Nazaré M; Rademacher C

ACS chemical biology 2018

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A new highly thyrotropin receptor-selective small molecule antagonist with potential for the treatment of Graves' orbitopathy.

  • Marcinkowski P; Hoyer I; Specker E; Furkert J; Rutz C; Neuenschwander M; Sobottka S; Sun H; Nazare M; Berchner-Pfannschmidt U; von Kries JP; Krause G

Thyroid : official journal of the American Thyroid Association 2018

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Use of a sequential high throughput screening assay to identify novel inhibitors of the eukaryotic SRP-Sec61 targeting/translocation pathway.

  • Klein W; Rutz C; Eckhard J; Provinciael B; Specker E; Neuenschwander M; Kleinau G; Scheerer P; von Kries JP; Nazaré M; Vermeire K; Schülein R

PloS one 2018

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Novel strategy for the preparation of 3-perfluoroalkylated-2H-indazole derivatives

  • Bel Abed, H.; Weißing, N.; Schoene, J.; Paulus, J.; Sewald, N.; Nazaré, M.

Tetrahedron Letters 2018

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Novel Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of P4 Substituents in Combination with a Neutral P1 Ligand.

  • Marc Nazare; et al. et al.

ChemInform 2004

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A Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones

  • Marc Nazaré; Claudia Schneider; Andreas Lindenschmidt; David William Will

Angewandte Chemie International Edition 2004

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Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.

  • Marc Nazaré

Bioorganic & medicinal chemistry letters 2004

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Factor Xa Inhibitors Based on a 2-Carboxyindole Scaffold: SAR of Neutral P1 Substituents.

  • Marc Nazare; et al. et al.

ChemInform 2004

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Eine flexible, palladiumkatalysierte Indol- und Azaindolsynthese durch direkte Anellierung von Chloranilinen und Chloraminopyridinen mit Ketonen

  • Marc Nazaré; Claudia Schneider; Andreas Lindenschmidt; David William Will

Angewandte Chemie 2004

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A Flexible, Palladium-Catalyzed Indole and Azaindole Synthesis by Direct Annulation of Chloroanilines and Chloroaminopyridines with Ketones.

  • Marc Nazare; Claudia Schneider; Andreas Lindenschmidt; David William Will

ChemInform 2004

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Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand

  • Marc Nazaré; Melanie Essrich; David W Will; Hans Matter; Kurt Ritter; Matthias Urmann; Armin Bauer; Herman Schreuder; Jörg Czech; Martin Lorenz; Volker Laux; Volkmar Wehner

Bioorganic & Medicinal Chemistry Letters 2004

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Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents

  • Marc Nazaré; Melanie Essrich; David W Will; Hans Matter; Kurt Ritter; Matthias Urmann; Armin Bauer; Herman Schreuder; Angela Dudda; Jörg Czech; Martin Lorenz; Volker Laux; Volkmar Wehner

Bioorganic & Medicinal Chemistry Letters 2004

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Portraitfoto: © Silke Oßwald