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Thursday, 19 November 2015

Boris Schmidt


Boris Schmidt

Prof. Dr.
  • Technical University Darmstadt
    Clemens Schöpf-Institute of Chemistry and Biochemistry
    Darmstadt, Hessen, Germany
    *Phone: +49 6151 163075. Fax: +49 6151 163278.
    E-mail: Schmidt_boris@t-online.de.

  • Medicinal Chemistry

    • Molecular mechanisms of neurodegenerative diseases: Alzheimer's disease, BSE
    • Protein aggregation: amyloid beta, tau, prions
    • Enzyme inhibition: aspartic proteases (Alzheimer's disease), 20 S proteasome (Oncology)

    Organic Synthesis

    • in Ionic Liquids
    • Aromatic heterocycles
    • Peptide mimetics

RESEARCH EXPERIENCE

  • Mar 2002–present
    Technische Universität Darmstadt · Clemens Schöpf Institut für Organische Chemie und Biochemie
    Germany · Darmstadt
  • May 1999–Feb 2002, Novartis, Novartis Pharma AG
    Switzerland · Basel
  • May 1994–Apr 1999
    Leibniz Universität Hannover · Institute of Organic Chemistry
    Germany · Hannover

AWARDS & ACHIEVEMENTS

  • Nov 2012
    Award: Hans AND Ilse Breuer Award Alzheimer Research

Contact

Darmstadt University of Technology Chemistry

Prof. Dr. Boris Schmidt
L2 | 02,458 Alaric-Weiss-Straße 4 64287 Darmstadt
+49 6151 16-3075

CV Prof. Schmidt


curriculum vitae

  • 1962 Born in San Fernando / Trinidad & Tobago
  • 1962-1965 Trinidad and Brazil
  • 1982-1989 Chemistry studies at the University of Hannover, Germany and Imperial College, London
  • 1991 Doctorate with Prof. HMR Hoffmann at the University of Hannover; Germany
  • 1991-94 Teacher at the Uppsala Biomedical Centre, Sweden
  • 1993 Postdoc with Prof. KB Sharpless, Scripps Research Institute, La Jolla, California
  • 1994-1999 Habilitation for Organic Chemistry at the University of Hannover, Germany
  • 1999-2002 Novartis Pharma AG, Basel, Switzerland, Central Nervous System Research
  • 2002 Associate (C3) professorship at the Darmstadt University of Technology

Awards

  • 1986 Scholarship for the Imperial College, London UK
  • 1991 Doctoral Prize of the Hoechst AG
  • 1991 PhD: Summa cum laude
  • 1992 German Research Foundation Fellowship
  • 1994 Uppsala University Fellowship, Sweden

Memberships

  • German Chemical Society
  • American Chemical Society
  • German Pharmaceutical Society
Office hours: Thu 10-12 clock "Whatever other perils humanity may face in the future did read ahead, boredom is not among them". Arthur C. Clarke str11 Cas 1820758-44-8 C24 H18 F N3 O4 S 4′-((5-(2,3-Dihydrobenzo[b][1,4]dioxin-6-yl)-1,3,4-oxadiazol-2-yl-thio)-methyl)-4-fluorobiphenyl-2-carboxamide NMR 1000 NMR 1001 Glycogen synthase kinase-3 (GSK-3) is a constitutively active, ubiquitous serine/threonine kinase that takes part in a number of physiological processes ranging from glycogen metabolism to apoptosis. GSK-3 is a key mediator of various signaling pathways, such as the Wnt and the insulin/AKT signaling pathways. Therefore, dysregulation of GSK-3 has been linked to various human diseases, such as cancer, diabetes, and neurodegenerative diseases.Two related isoforms of GSK-3 exist in mammals, GSK-3α and -β, which share a sequence identity within their catalytic domains of 98%. Beyond the catalytic domains they show significant differences. Although these isoforms are structurally related, they are not functionally equivalent, and one cannot compensate for loss of the other. The debate on the respective contributions of the isoforms GSK-3α and GSK-3β on the pathogenesis of different diseases is ongoing. Various studies indicate that the therapies of certain diseases benefit from specific targeting of GSK-3α and GSK-3β. GSK-3α was recently identified as a differentiation target in acute myeloid leukemia (AML). AML is a hematopoietic malignancy defined by uncontrolled proliferation and disrupted myeloid differentiation. AML is the second most common form of leukemia in adults. The current treatment of AML with conventional chemotherapy is very aggressive yet ineffective for the majority of patients with the disease.Thus, alternative targeted treatment approaches for AML are highly desirable. GSK-3α recently emerged as a potential target in this disease.

PAPER

Abstract Image
The challenge for glycogen synthase kinase-3 (GSK-3) inhibitor design lies in achieving high selectivity for one isoform over the other. The therapy of certain diseases, such as acute myeloid leukemia (AML), may require α-isoform specific targeting. The scorpion shaped GSK-3 inhibitors developed by our group achieved the highest GSK-3α selectivity reported so far but suffered from insufficient aqueous solubility. This work presents the solubility-driven optimization of our isoform-selective inhibitors using a scorpion shaped lead. Among 15 novel compounds, compound 27 showed high activity against GSK-3α/β with the highest GSK-3α selectivity reported to date. Compound 27 was profiled for bioavailability and toxicity in a zebrafish embryo phenotype assay. Selective GSK-3α targeting in AML cell lines was achieved with compound 27, resulting in a strong differentiation phenotype and colony formation impairment, confirming the potential of GSK-3α inhibition in AML therapy

Evaluation of Improved Glycogen Synthase Kinase-3α Inhibitors in Models of Acute Myeloid Leukemia

† Clemens Schöpf Institute of Organic Chemistry and Biochemistry, Technische Universität Darmstadt, 64287 Darmstadt, Germany
‡ Department of Pediatric Oncology, Dana-Farber Cancer Institute, Harvard Medical School, Boston, Massachusetts 02215, United States
J. Med. Chem., Article ASAP
DOI: 10.1021/acs.jmedchem.5b01200
Publication Date (Web): October 23, 2015
Copyright © 2015 American Chemical Society
*Phone: +49 6151 163075. Fax: +49 6151 163278. E-mail: Schmidt_boris@t-online.de.
http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b01200
http://pubs.acs.org/doi/suppl/10.1021/acs.jmedchem.5b01200/suppl_file/jm5b01200_si_001.pdf
compound 27 as a colorless solid. HPLC: 96%, tR = 6.93 min.
1H NMR (DMSO-d6, 500 MHz, 300 K): δ (ppm) = 4.32 (td, J = 5.2 Hz, J = 3.7 Hz, 4H), 4.60 (s, 2H), 7.05 (d, J = 8.4 Hz, 1H), 7.25 (dd, J = 9.1 Hz, J = 2.7 Hz, 1H), 7.31 (td, J = 8.6 Hz, J = 2.8 Hz, 1H), 7.38 (m, 3H), 7.41 (d, J = 2.0 Hz, 1H), 7.45 (dd, J = 8.4 Hz, J = 2.1 Hz, 1H), 7.49 (d, J = 8.2 Hz, 2H), 7.73 (s, 1H).
13C NMR (DMSO, 125 MHz, 300 K): δ (ppm) = 35.6, 64.1, 64.4, 114.3 (d, JC–F = 21 Hz), 115.0, 115.9 (d, JC–F = 21 Hz), 115.9, 118.1, 120.0, 128.6 (2C), 128.8 (2C), 132.0 (d, JC–F = 8 Hz), 134.8, 135.5, 138.9, 139.0 (d, JC–F = 7 Hz), 143.8, 146.7, 160.9 (d, JC–F = 247 Hz), 162.7, 164.9, 169.5.
EI-MS: m/z = 463 (100, [M+]), 464 (26, [M+ + H]), 465 (7, [M+ + 2H].

Publications in peer reviewed journals

Reaction mechanism, methods, synthesis

1. Hoffmann, H. M. R.; Schmidt, B.; Wolff, S. Preparation of 5-Bromotetronates [4-Alkoxy-5-bromo-2(5H)-furanones] and a New Concept for the Synthesis of Aflatoxins and Related Structure Types. Tributyltin Hydride versus Palladium-Promoted Intramolecular Hydroarylation. Tetrahedron, 1989, 45, 6113-6126.
2. Hoffmann, H. M. R.; Schmidt, B. Progress Towards a Convergent and Flexible Synthesis of AFM1. J. Toxicol.-Toxin Reviews, 1989, 8, 299-304
3. Schmidt, B.; Hoffmann, H. M. R. On the Way to Aflatoxins and Related Structure Types. Regio-controlled Annelations by Application of Homogenous Palladium Catalysis, Urethane Tether and ortho, ortho’-Diiodine Effect. Tetrahedron, 1991, 47, 9357-9368. (IF 3.40)
4. Schmidt, B.; Hoffmann, H. M. R. Regioselective Preparation of Iodinated Phloroglucinols. Chem. Ber.,1992, 125, 1501-1506
5. Schmidt, B.; Chelidonic Acid as Precursor for 2,5-Desoxy-C-glycosides. Heterocycles, 1999, 51, 179-182
6. R. Raecker, M. Nicholas, B. Schmidt, O. Reiser; First determination of an activation volume for the osmium-catalyzed dihydroxylation of an alkene. J. Chem. Soc. Perk. Trans 2, 1999, 1615-1617. Räcker, Reinhard; Nicolas, Muriel; Schmidt, Boris; Reiser, Oliver. First determination of an activation volume for the osmium-catalyzed dihydroxylation of an alkene. J. Chem. Soc., Perkin Trans. 2, 1999, 2653
7. Schmidt, B.; Kühn, C. 2-Mercaptopyridine – Activated Thioates and Ketene Thioacetals. J. Prakt. Chem.1999, 341 (2), 114-120. ttp:www.wiley-vch.de/contents/jc_2258/199902.html
8. H. A. Braun, R. Meusinger, B. Schmidt, 2-Iodoethanols from aldehydes, diiodomethane and isopropyl-magnesium Chloride, Tetrahedron Lett., 2005, 46 (15), 2551-2554
9. Umbreen, S.; Foro, S.; Schmidt, B., (S)-4-[2-(3-Cyanobenzamido)-3-hydroxypropyl]phenyl 3-cyano-benzoate. Acta Crystallographica, Section E: Structure Reports Online, 2006, 62(6), o2551-2552
10. Everson da Silva, L.; Joussef, A.C.; Foro, S.; Schmidt, B., 5-(Aminomethylene)-2,2-dimethyl-1,3-dioxane-4,6-dione. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(9), o3866-o3867
11. Everson da Silva, L.; Joussef, A.C.; Foro, S.; Schmidt, B., 4-n-Propyl-N-(8-quinolyl)benzenesulfonamide. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(9), o3606-o3607
12. B. Schmidt, D. Meid, D. Kieser, Safe and Fast Tetrazole Formation in Ionic Liquids, Tetrahedron, 2007, 63, 492-496. http://dx.doi
13. A. Zall, D. Bensinger, B. Schmidt, Oxidative homologation of aldehydes to a-ketoaldehydes by iodoform, IBX and dimethylsulfoxide. Eur. J. Org. Chem. 2012 online 24.1.2012

Angiotensin II/Peptidomimetics

14. Schmidt, B.; Lindman, S.; Tong, W.; Lindeberg, G.; Gogoll, A.; Lai, Z.; Thörnwall, M.; Synnergren, B.;Nilsson, A.; Welch, C. J.; Sohtell, M.; Westerlund, C.; Nyberg, F.; Karlén, A.; Hallberg, A. Design, Synthesis and Biological Activities of Four Angiotensin II Receptor Ligands with ϒ-Turn Mimetics Replacing Amino Acid Residues 3-5. J. Med. Chem, 1997, 40, 903-919.
15. Kühn, C.; Lindeberg, G.; Gogoll, A.; Hallberg, A.; Schmidt, B.; Fmoc Protected Peptide Mimetic Based on a Cyclohexane Framework and Incorporation into Angiotensin II. Tetrahedron, 1997, 53, 12497-12504
16. Schmidt, B.; Kühn, C.; Racemic, Yet Diasteromerically Pure Azido Acids as Both ϒ-Turn and Inverse ϒ-Turn Mimetics for Solid-Phase Peptide Synthesis, Synlett, 1998, 1240
17. Schmidt, B.; Patzke G. R. Fmoc-N-allyl Glycine Derived N-Allyl-2,5-diketopiperazines. Synthetic Communications, 1999, 29(6), 1025-1032
18. B. Schmidt, C. Kühn, D.K. Ehlert, G. Lindeberg, S. Lindman, A. Karlén, A. Hallberg, A Frame Shifted Disulfide Bridged Analogue of Angiotensin II. Bioorg. Med. Chem., 2003, 11, 985-990

Sartane metabolism

19. Kramer, C., J. Sunkomat, B. Schmidt, B, Schieffer et al.. Angiotensin II Receptor-Independent Antiinflammatory and Antiaggregatory Properties of Losartan. Role of the Active Metabolite EXP3179.Circulation Research, 2002, 770-77
20. B. Schieffer, B. Schmidt, H. Drexler, Angiotensin-II-Rezeptor-unabhängige anti-inflammatorische und antiaggregatorische Eigenschaften von AT1-Antagonisten. Rolle aktiver Metaboliten. Herz BNK, 2003, 28 (7), 2
21. M. Schupp, L. D. Lee, N. Frost, S. Umbreen, B. Schmidt, T. Unger, U. Kintscher. CHBPR-Regulation of PPARg Activity by Losartan Metabolites. Hypertension, 2006, 47(3), 586-9
22. C. Grothusen, S. Umbreen, I. Konrad, K. Stellos, C. Schulz, B. Schmidt, E. Kremmer, O. Teebken, S. Massberg, M. Luchtefeld, B. Schieffer*, M. Gawaz. EXP3179 Inhibits Collagen-Dependent Platelet Activation via Glycoprotein Receptor-VI Independent of AT1-Receptor Antagonism. Arteriosclerosis, Thrombosis & Vascular Biology, 2007, 27(5), 1184-1190
23. L. Danielyan*, A. Lourhmati, S.Verleysdonk, B. Proksch, S.Umbreen, B. Schmidt, C.H. Gleiter. Angiotensin receptor type 1 blockade in astrocytes decreases hypoxia-induced cytotoxicity and inflammation. Neurochemical Research, 2007, 9, 1489-1498.
24. D. Werner, U. Werner, A. Meybaum, B. Schmidt, S. Umbreen, A. Grosch, H. G. Lestin, B. Graf, O. Zolk; M.F. Fromm. Determinants of steady-state torasemide pharmacokinetics: Impact of gender, pharmacogenetic factors and angiotensin II receptor blockers. Clinical Pharmacokinetics, 2008, 47(5), 323-32. (IF 4.12) 20 S Proteasome

20 S Proteasome

25. B. Schmidt, Hannes A. Braun, E-1,2-Dichlorovinyl ethers as irreversible protease inhibitors. Tet. Lett,2004, 45 (8), 1751-1753
26. H. A. Braun, S. Umbreen, M. Groll, U. Kuckelkorn, I. Mlynarczuk, M. E. Wiegand, I. Drung, P. M. Kloetzel, B. Schmidt. Tripeptide mimetics inhibit the 20S proteasome by covalent bonding to the active site threonines J. Biol Chem, 2005, 280 (31), 28394-28411
27. I. Mlynarczuk-Bialy, H. Roeckmann, U. Kuckelkorn, B. Schmidt, S. Umbreen, J. Golab, A. Ludwig, C. Montag, L. Wiebusch, C Hagemeier, D. Schadendorf, P.-M. Kloetzel, U. Seifert. Combined Effect of Proteasome and Calpain Inhibition on Cisplatin-Resistant Human Melanoma Cells. Cancer Research, 2006, 66(15), 7598-7605
28. M.A. Graewert, N. Gallastegui, M. Stein, B. Schmidt, P.-M. Kloetzel, R. Huber, M. Groll. Elucidation of the α-Keto-Aldehyde Binding Mechanism: A Lead Structure Motif for Proteasome Inhibition. Angew. Chemie 2011, 123(2), 563-566, Angew. Chemie IE, 2011, 50(2), 542-546

Alzheimer Dementia

29. B. Schmidt, A. Zall, G. Larbig, Inhibitors Designed for Presenilin 1 by Means of Aspartic Acid Activation. Helvetica Chimica Acta , 2004, 87, 2334-2340
30. B. Schmidt, S. Baumann, R. Narlawar, H.A. Braun, G. Larbig. Modulators and Inhibitors of ϒ- and β-Secretase. Neurodegenerative Diseases, 2006, 3(4-5), 290-297
31. G. Larbig, B. Schmidt. A Facile Synthesis of Tetramic & Tetronic Acids as β-Secretase Inhibitors, J. Combinatorial Chemistry , 2006, 8, 480-490
32. S. Umbreen, M. Brockhaus, H. Ehrenberg, B. Schmidt. Norstatines from Aldehydes by Sequential Organocatalytic α-Amination and Passerini Reaction. European J. Org. Chem. 2006, 4585-4595
33. R. Narlawar, K.-H. Baumann, R. Schubenel, B. Schmidt. Curcumin Derivatives inhibit or modulate β-amyloid precursor protein metabolism. Neurodegen. Dis. 2007, 4(2), 88-93
34. R. Narlawar, B. Perez Revuelta, K. Baumann, R. Schubenel, C. Haass, H. Steiner, B. Schmidt*. N-Substituted Carbazolyloxyacetic Acids Modulate Alzheimer Associated ϒ–Secretase. Biorg. Med. Chem. Lett. 2007, 17(1), 176-182
35. R. Narlawar, B. Perez Revuelta, C. Haass, H. Steiner, K.-H. Baumann, B. Schmidt*. The Scaffold of the COX-2 Inhibitor Carprofen Provides Alzheimer ϒ-Secretase Modulators. J. Med. Chem. 2006, 49(26), 7588-7591
36. G. Larbig, M. Pickhardt, D.G. Lloyd, B. Schmidt*, E. Mandelkow. Screening for inhibitors of tau protein aggregation into Alzheimer paired helical filaments: A ligand based approach results in successful scaffold hopping. Current Alzheimer Research 2007, 4(3), 315-323
37. V. Limongelli, L. Marinelli*, S. Cosconati, H. A. Braun, B. Schmidt, E. Novellino. Ensemble-docking approach on BACE-1: Pharmacophore Perception and Directives for Drug Development. ChemMedChem,2007, 2(5), 667-678
38. M. Pickhardt, G. Larbig, I. Khlistunova, A. Coksezen, B. Meyer, E-M. Mandelkow, B. Schmidt*, E. Mandelkow*. Phenylthiazolyl-hydrazide and its derivatives are potent inhibitors of tau aggregation and toxicity in vitro and in cells. Biochemistry, 2007, 46(35), 10016 -10023
39. R. Narlawar, K. Baumann, C. Czech, B. Schmidt. Conversion of the LXR-Agonist TO-901317 – From Inverse to Normal Modulation of g-Secretase by Addition of a Carboxylic Acid and a Lipophilic Anchor.Biorg. Med. Chem. Lett. 2007, 17(19), 5428-5431
40. H. A. Braun, A. Zall, M. Brockhaus, M. Schütz, R. Meusinger, B. Schmidt. Aspartic Protease Inhibitors via C1 -Homologation of Peptidic Aldehydes and Studies on Reduced Amide Isosteres. Tet. Lett. 2007, 48(45) 7990-7993
41. R. Narlawar, M. Pickhardt, S. Leuchtenberger, K. Baumann, S. Krause, T. Dyrks, S. Weggen, E. Mandelkow, B. Schmidt*. Curcumin Derived Pyrazoles and Isoxazoles – Swiss Army Knives or Blunt Tools for Alzheimer´s Disease? ChemMedChem, 2008, 3, 165-172
42. T. L. Kukar, T. B. Ladd, M. A. Bann, P. C. Fraering, R. Narlawar, G. M. Maharvi, B. Healy, R.Chapman, A. Welzel, R. W. Price, B. Moore, V. Rangachar, B. Cusack, J. Eriksen, K. Jansen-West, C. Verbeeck, D. Yager, C. Eckman, W. Ye, S. Sagi, B. A. Cottrell, J.Torpey, T. L. Rosenberry, A. Fauq, M. S. Wolfe, B. Schmidt, D. M. Walsh, Edward H. Koo, T.E. Golde. Substrate targeting ϒ-Secretase Modulators. Nature, 2008, 453, 7197
43. S. Baumann, N. Hoettecke R. Schubenel, K. Baumann, B. Schmidt. NSAID-derived ϒ-secretase modulators. Part III. Membrane anchoring. Biorg. Med. Chem. Lett. 2009, 19 (24), 19, 6986-6990
44. J. Pruessmeyer, C. Martin, F. M. Hess, N. Schwarz, S. Schmidt, T. Kogel, N. Hoettecke, B. Schmidt, A. Sechi, S. Uhlig, A. Ludwig. A Disintegrin and Metalloproteinase 17 (ADAM17) Mediates Inflammation-induced Shedding of Syndecan-1 and -4 by Lung Epithelial Cells. J. Biol. Chem. 2010, 285(1), 555-564
45. N. Hoettecke, A. Ludwig, S. Foro, B. Schmidt. Improved Synthesis of ADAM10 Inhibitor GI254023X.Neurodegenerative Diseases, 2010, 7(4), 232-238
46 N. Hoettecke, M. Liebeck, K. Baumann, R. Schubenel, E. Winkler, H. Steiner, B. Schmidt. Inhibition of ϒ-secretase by the CK1 inhibitor IC261 does not depend on 1d, Biorg. Med. Chem. Lett. 2010, 20(9), 2958-2963
47. S. Burgold, T. Bittner, M. M. Dorostkar, D.Kieser, M. Fuhrmann, G. Mitteregger, H. Kretzschmar, B. Schmidt, J. Herms. In vivo multiphoton imaging reveals gradual growth of newborn amyloid plaques over weeks Acta Neuropathologica, 2011, 121, 327-335
48. F. Lo Monte, T. Kramer, A. Boländer, B. Plotkin, H. Eldar-Finkelman, A. Fuertes, J. Dominguez, B. Schmidt. Synthesis and biological evaluation of glycogen synthase kinase 3 (GSK-3) inhibitors: a fast and atom efficient access to 1-aryl-3-benzylureas. Bioorg. Med. Chem. Lett. 2011, 21(18), 5610-5615
49. A. Zall, D. Kieser, N. Höttecke, E. C. Naumann, B. Thomaszewski, K. Schneider, D.T. Steinbacher, R. Schubenel, S. Masur, K. Baumann, B. Schmidt. NSAID-derived ϒ-secretase modulation requires an acidic moiety on the carbazole scaffold. Bioorg. Med. Chem. 2011, 19(16), 4903-4911
50. A. Taghavi, S. Nasir, M. Pickhardt, R. Heyny-von Haußen, G. Mall, E. Mandelkow, E.-M. Mandelkow, B. Schmidt. N'-benzylidene-benzohydrazides as novel and selective tau-PHF ligands. J. Alzheimer’s Disease,2011, 27 (4), 835-843
51. F. Lo Monte, T. Kramer, J. Gu, U. Anumala, L. Marinelli, V. La Pietra, E. Novellino, B. Franco, D. Demedts, F. Van Leuven, A. Fuertes, J. Dominguez, B. Plotkin, H. Eldar-Finkelman, B. Schmidt.Identification of Glycogen Synthase Kinase-3 Inhibitors with a Selective Sting for Glycogen Synthase Kinase-3α. J. Medicinal Chemistry, 2012, 55 (9), 4407–4424
52. A. Boländer, D. Kieser, C. Voss, S. Bauer, C. Schön, S. Burgold, T. Bittner, J. Hölzer, R. Heyny-von Haußen, G. Mall, V. Goetschy, C. Czech, H. Knust, R. Berger, J. Herms, I. Hilger, B. Schmidt. Bis(arylvinyl)pyrazines, -pyrimidines and -pyridazines as Imaging Agents for Tau Fibrils and β-Amyloid Plaques in Alzheimer’s Disease Models. J. Med. Chem. 2012, 55 (21), 9170-9180
53. T. Bittner, S. Burgold, M. M. Dorostkar, M. Fuhrmann, B. M. Wegenast-Braun, B. Schmidt, H. Kretzschmar, J. Herms. Amyloid plaque formation precedes dendritic spine loss. Acta Neuropathologica,2012, 124 (6), 797-808
54. J. Gu, U. R. Anumala, F. Lo Monte, T. Kramer; R. Heyny-von Haußen, J. Hölzer; V. Goetschy-Meyer; G. Mall, I. Hilger, C. Czech, B. Schmidt. 2-Styrylindolium based fluorescent probes visualize neurofibrillary tangles in Alzheimer's disease. Bioorg. Med. Chem. Lett. 2012, 22 (24), 7667-7671
55. C. Schön, N.A. Hoffmann, S.M. Ochs, S. Burgold, S. Filser, S. Steinbach, M.W. Seeliger, T. Arzberger, M. Goedert, H.A. Kretzschmar, B.Schmidt, J. Herms. Long-Term In Vivo Imaging of Fibrillar Tau in the Retina of P301S Transgenic Mice. PLoS ONE, 2012, 7(12): e53547. doi:10.1371/journal.pone.0053547
56. F. Lo Monte, T. Kramer, J. Gu, M. Brodrecht, J. Pilakowski, Ana Fuertes, J. M. Dominguez, B. Plotkin, H. Eldar-Finkelman, B. Schmidt, Structure-based optimization of oxadiazole-based GSK-3 inhibitors.European J. Med. Chem. 2013, 61, 26-40
57. J. Gu, U.R. Anumala, R. Heyny-von Haußen, J. Hölzer, V. Goetschy-Meyer, G. Mall, I. Hilger, C. Czech, B. Schmidt. Design, Synthesis and Biological Evaluation of Trimethine Cyanine Dyes as Fluorescent Probes for the Detection of Tau Fibrils in Alzheimer´s Disease Brain and Olfactory Epithelium. ChemMedChem,2013, 8, 891-897
58. A. Boländer, D. Kieser, C. Scholz, R. Heyny-von Haußen, G. Mall, V. Goetschy, C. Czech B. Schmidt. Synthesis of Methoxy-X04 Derivatives and their Evaluation in Alzheimer's Disease Pathology.Neurodegenerative Diseases, 2013, accepted 18.4.2013
59. E. C. Naumann, S. Göring, I. Ogorek, S. Weggen, B. Schmidt. Membrane anchoring ϒ-secretase modulators with terpene-derived moieties. Bioorg. Med. Chem. Lett. 2013, 23, 3852-3856
60.

Trypanosoma

61. Luiz Everson da Silva, Antônio Carlos Joussef, Letícia Kramer Pacheco, Daniela Gaspar da Silva, Mário Steindel, Ricardo Andrade Rebelo and Boris Schmidt, Synthesis and in vitro evaluation of leishmanicidal and trypanocidal activities of N-quinolin-8-yl-arylsulfonamides. Bioorg. Med. Chem. 2007, 15, 7553–7560. Cystic fibrosis / protein folding / natural products

Cystic fibrosis / protein folding / natural products

62. Karen Bernard, Wei Wang, Rajeshwar Narlawar, Boris Schmidt, Kevin L. Kirk. Curcumin cross-links cystic fibrosis transmembrane conductance regulator (CFTR) polypeptides and potentiates CFTR channel activity by distinct mechanisms. J. Biol. Chem. 2009, 284, 30754-3076

Co-authored ADAM 10 related publications

63. Alison M. Cooper, Philip S. Hobson, Mark R. Jutton, Michael W. Kao, Binia Thomaszewski, Boris Schmidt, David J. Fear, Andrew J. Beavil, James M. McDonnell, Brian J. Sutton & Hannah J. Gould. Soluble CD23 Controls IgE Synthesis and Homeostasis in Human B Cells. J. of Immunology, 2012, 188 (7), 3199-3207
64. V. Lo Sardo, C. Zuccato, G. Gaudenzi, B. Vitali, C. Ramos, M. Tartari, M.A. Myre, J.A. Walker, A. Postocchi, L. Conti, M. Valenza, B. Drung, B. Schmidt, J. Gusella, S. Zeitlin, F. Cotelli, E. Cattaneo. Nature Neuroscience, 2012, An evolutionary recent neuroepithelial cell adhesion function of huntingtin implicates ADAM10-Ncadherin, 15 (5), 713-721. (IF 14.19)
65. Q. Xiao, F. Zhang, L. Lin, C. Fang, G. Wen, T.-N. Tsai, X. Pu, D. Sims, Z. Zhang, X. Yin, B. Thomaszewski, B. Schmidt. M. Mayr, K. Suzuki, Q. Xu, S. Ye. A Functional Role of Matrix Metalloproteinase-8 in Stem/Progenitor Cell Migration and Their Recruitment into Atherosclerotic Lesions. Circulation Research,2013, 112, 35 (IF 9.9).
66. Q. Xiao, F. Zhang, G. Grassia, Y. Hu, Z. Zhang, Q. Xing, X. Yin, M. Maddaluno, B. Drung, B. Schmidt, P. Maffia, A. Ialenti, M. Mayr, Q. Xu, S. Ye. Matrix Metalloproteinase-8 Promotes Vascular Smooth Muscle Cell Proliferation and Neointima Formation. Arterioscler. Thromb. Vasc. Biol. 2013, published online October 24 2013, (IF 6.338) doi:10.1161/ATVBAHA.113.301418

Kinase inhibition

67. Amombo, G. M. O.; Kramer, T.; Lo Monte, F.; et al.. Modification of a promiscuous inhibitor shifts the inhibition from gamma-secretase to FLT-3 . Bioorganic & Medicinal Chemistry Letters, 2012, 22 (24), 7634-7640

Metal complexes / X-ray structure determination

68. Schmidt, B.; Neitemeier V.; 6-Pyridylnicotine – A New Chiral 2,2’-Bipyridine. Synthesis, 1998, 42. (IF 2.2)
69. Schmidt, B.; Ehlert, D. K.; Preparation of N-Boc-(2,6-bis(ethoxycarbonylpyridiny-4-yl)-L-alanines as tridentate ligands. Tet. Lett. 1998, 39, 3999-4002
70. G. Muller, B. Schmidt, J. Jiricek, G. Hopfgartner, J.P. Riehl, J.C.G. Buenzli, C. Piguet. Lanthanide triple helical complexes with a chiral ligand derived from 2,6-pyridindicarboxylic acid. J.Chem. Soc., Dalton Trans. 2001, 2658-2665
71. G. Muller, B. Schmidt; J. Jiricek, J.C.G. Buenzli, K.J. Schenk. 3-[2,6-Bis(diethylcarbamoyl)-pyridin-4-yl]-N-(tert-butoxycarbonyl)alanine methyl ester: a chiral tridentate ligand that causes a diastereomeric excess of its lanthanide complexes in solution. Acta Crystallographica, Section C: Crystal Structure Communications, 2003, 59, 353-356
72. B. Schmidt, A. Titz, J. Jiricek, Guofeng Ye, K. Parang, Copper dipicolinates as peptidomimetic ligands for the Src SH2 domain. Bioorg. Med. Chem. Lett. 2004, 14 (16), 4203-4206
73. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 6-Nitroquinolin-2(1H)-one. Acta Crystallographica, Section E: Structure Reports Online, 2005, E61(9), 2992-2993
74. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 4-Fluoro-N-(quinolin-8-yl)benzenesulfonamide. Acta Crystallographica, Section E: Structure Reports Online, 2005, E61(12), o4387-o4388
75. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., N-Benzyl-8-nitroquinolin-2-amine. Acta Crystallographica, Section E: Structure Reports Online, 2005, E61(11), o3837-o3838
76. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., N-(5,7-Dibromo-8-quinolyl)-4-fluorobenzenesulfonamide. Acta Crystallographica, Section E: Structure Reports Online, 2005, E61(11), o3782-o3783
77. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 2,4,6-Triisopropyl-N-(8-quinolyl)benzenesulfonamide. Acta Crystallographica, Section E: Structure Reports Online, 2005, E61(11), o3780-o3781
78. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 4-Nitro-N-(8-quinolyl)benzenesulfonamide.Acta Crystallographica, Section E: Structure Reports Online, 2005, E61(11), o3778-o3779
79. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 5,7-Dibromo-N-tosylquinolin-8-amine. Acta Crystallographica, Section E: Structure Reports Online, 2005, E61(10), o3435-o3436
80. Everson da Silva, L. E.; Joussef, A. C.; Foro, S.; Schmidt, B., N-(6-Methoxy-2-methyl-8-quinolyl)-4-n-propylbenzenesulfonamide. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(2), o626-o627
81. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 2,2-Dimethyl-5-[(6-methylpyridin-2-yl-amino)-methylene]-1,3-dioxane-4,6-dione. Acta Crystallographica, Section E: Structure Reports Online,2006, E62(8), o3477-o3478
82. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 2,2-Dimethyl-5-[(4-p-tolylthiazol-2-ylamino)-methylene]-1,3-dioxane-4,6-dione. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(8), o3215-o3216
83. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Bis[N-(5,7-dibromoquinolin-8-yl)-3,5-bis(trifluoro-methyl)benzenesulfonamidato-k2N,N']zinc(II). Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(8), m1901-m1903
84. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Aquabis[4-nitro-N-(quinolin-8-yl)benzenesulfonamidato-k2N,N']zinc(II). Acta Crystallographica, Section E: Structure Reports Online,2006, E62(8), m1773-m1775
85. Everson da Silva, L.; Joussef, A. C.; Silva, L. L.; Foro, S.; Schmidt, B., 4-n-Propyl-N-(8-quinolyl)-benzene-sulfonamide. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(9), o3606-o3607
86. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., N-(5,7-Dibromo-8-quinolyl)-3,5-difluoro-benzenesulfonamide. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(7), o2630-o2631
87. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Bis[4-fluoro-N-(quinolin-8-yl)benzenesulfonamidato-k2N,N']zinc(II) hemihydrate. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(7), m1719-m1721
88. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Aquabis[N-(5,7-dibromoquinolin-8-yl)-4-methylbenzenesulfonamidato-k2N,N']zinc(II). Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(6), m1258-m1259
89. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 5-{[4-(4-Bromophenyl)thiazol-2-yl]amino-methylene}-2,2-dimethyl-1,3-dioxane-4,6-dione. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(5), o1722-o1723
90. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Bis[4-n-propyl-N-(8-quinolyl)benzenesulfonamidato-k2N,N']zinc(II) dimethylformamide solvate. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(5), m999-m1001
91. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Bis[2,4,6-triisopropyl-N-(quinolin-8-yl)-benzene-sulfonamidato-k2N,N']copper(II). Acta Crystallographica, Section E: Structure Reports Online,2006, E62(4), m912-m913.
92. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 2-(1,3-Benzothiazol-2-yl)quinolin-8-ol. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62, (3), o880-o881
93. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Bis[4-nitro-N-(quinolin-8-yl)benzenesulfonamidato-k2N,N'']copper(II). Acta Crystallographica, Section E: Structure Reports Online,2006, E62(3), m518-m519.
94. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Bis[2,4,6-triisopropyl-N-(quinolin-8-yl)-benzenesulfonamidato-k2N,N']zinc(II). Acta Crystallographica, Section E: Structure Reports Online,2006, E62(3), m516-m517
95. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 5-[(6-Fluoro-1,3-benzothiazol-2-ylamino)-methylene]-2,2-dimethyl-1,3-dioxane-4,6-dione. Acta Crystallographica, Section E: Structure Reports,2006, E62 (2), o742-o743.
96. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 4,5-Dibromo-N-(8-quinolyl)thiophene-2-sulfonamide. Acta Crystallographica, Section E: Structure Reports Online,2006, E62(1), o309-o310
97. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 2,2-Dimethyl-5-[(6-methylpyridin-2-yl-amino)-methylene]-1,3-dioxane-4,6-dione. Acta Crystallographica, Section E: Structure Reports Online,2006, E62(8), o3477-o3478
98. E. Ramic, R.-A. Eichel, K.-P. Dinse, A. Titz, B. Schmidt, Complexation of copper(II)-chelidamate – A multi-frequency pulsed Electron Paramagnetic Resonance and Electron Nuclear Double Resonance analysis J. Phys.Chem. 2006, 110(41), 20655-20663
99. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Bis[4-fluoro-N-(quinolin-8-yl)benzenesulfonamidato-k2N,N']copper(II) dichloromethane hemisolvate. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(7), m1606-m1608
100. Everson da Silva, L.; Joussef, A. C.; Rebelo, R.A.; Foro, S.; Schmidt, B., 2-Aminoquinolin-4-yl 2,4,6-triisopropylbenzenesulfonate. Acta Crystallographica, Section E: Structure Reports Online, 2006, E62(7), o5421–o5422.
101. Everson da Silva, L.; Joussef, A. C.; Rebelo, R.A.; Foro, S.; Schmidt, B., 2-Aminoquinolin-8-yl p-toluenesulfonate. Acta Crystallographica, Section E: Structure Reports Online, 2007, E63, o72–o74
102. Everson da Silva, L.; Joussef, A. C.; Rebelo, R.A.; Foro, S.; Schmidt, B., Aquabis(2-methylquinolin-8-olato-k2N,O)-zinc(II). Acta Crystallographica, Section E: Structure Reports Online, 2007, E63, m129–m132
103. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., Silva, 2-Aminoquinolin-8-yl-4-fluorobenzenesulfonate. Acta Crystallographica, Section E: Structure Reports Online, 2007, E63(1), o407-o408
104. Everson da Silva, L.; Joussef, A. C.; Foro, S.; Schmidt, B., 2-Aminoquinolin-8-yl-2,4,6-triisopropylbenzenesulfonate. Acta Crystallographica, Section E: Structure Reports Online, 2007, E63(1), o409-o411
105. Everson da Silva, L.; Foro, S.; Schmidt, B., 2-Aminoquinolin-8-yl 3,5-difluorobenzenesulfonate. Acta Crystallographica, Section E: Structure Reports Online, 2007, 63(2), o829-o830

Reviews in peer reviewed journals/series

106. B. Schmidt, Methyltrioxorhenium – From Oxidation and Cyclopropanation to Metathesis. J. Prakt. Chem. 1997, 339, 493-504
107. B. Schmidt, Aspartic Proteases involved in Alzheimer's disease, ChemBioChem, 2003, 4 (5), 367-378. (Impact factor 2.9)
108. B. Schmidt, B. Schieffer, Angiotensin II AT1 Receptor Antagonists: Clinical Implications of Active Metabolites. J. Med. Chem. 2003, 46, 2261. (Impact factor 5.3)
109. B. Schmidt, H. Drexler, B. Schieffer, Therapeutic Effects of Angiotensin (AT1) Receptor Antagonists: Potential Contribution of Mechanisms Other Than AT1 Receptor Blockade. American Journal of Cardiovascular Drugs, 2004, 4, 361-368
110. B. Schmidt, R. Narlawar, H. Braun, Drug Development and PET-Diagnostics for Alzheimer's Disease. Current Medicinal Chemistry. 2005, 12, 1677-1695
111. B. Schmidt, S. Baumann, H.A. Braun, G. Larbig, Inhibitors and Modulators of β- and ϒ-Secretase.Current Topics in Medicinal Chemistry. 2006, 6(4), 377-392
112. B. Bulic, M. Pickhardt, B. Schmidt, E.M. Mandelkow, H. Waldmann, E. Mandelkow. Development of Tau Aggregation Inhibitors for Alzheimer's Disease. Angew. Chem. Int. Ed. Engl. 2009, 48, 1740
113. T. Kramer, F. Lo Monte, S. Göring, G.M. Okala Amombo, B. Schmidt, Small molecule kinase inhibitors for LRRK2 and their application to Parkinson´s disease models. ACS Chemical Neuroscience 2012, 3(3), 151-160
114. T. Kramer, B. Schmidt, F. Lo Monte, International Journal of Alzheimer's Disease, Small-molecule inhibitors of GSK3 – Structural insights and their application to Alzheimer´s disease models, 2012, accepted. 31.1.2012
115. Schulz, S. Göring, B. Schmidt, C. Hopf, LRRK2 Kinase Inhibitors as New Drugs for Parkinson’s Disease? in Emerging Drugs and Target for Parkinson’s Disease, RSC Drug Discovery Series No. 34, 2013, p. 266-293. Ed. Ana Martinez, Carmen Gil. RSC Publishing, Cambridge, UK. ISBN: 978-1-84973-617-6

Monographies, books and other publications

116. Schmidt, B. Auf dem Weg zum Aflatoxin M1 und verwandten Strukturen durch homogene Katalyse, Dissertation, Universität Hannover 1991
117. B. Schmidt, V. Neitemeier, D.K. Ehlert, A. Backhaus-Ehlert, 6-Pyridylnicotines and 2,6-Pyridyl-dicarboxylates for Supramolecular Chemistry, no. 008 “Electronic Conference on Heterocyclic Chemistry 98”: H.S. Rzepa, O. Kappe (Eds), Imperial College Press, 1998, ISBN 81-02-3594-1,http://www.ch.ic.ac.uk/ectoc/echet98/pub/008/index.ht
118. Workshop of Young European Bio-Organic Chemists: Ed.: Ludger A. Wessjohann, Koeln : Prosciencia-Verl.-Buchh., Philipp, 1998, ISBN 3-932265-01-7
119. Schmidt, B. Biomimetika – Ihre Synthese durch Übergangsmetall-katalysierte Schlüssel-Reaktionen und ihre Anwendung; Habilitationsschrift, Universität Hannover 1998
120. B. Schmidt, A. Siegler. Aspartic Proteases involved in Alzheimer's disease, Highlights in Bioorganic Chemistry, ed. C. Schmuck, H. Wennemers. ISBN 3-527-30656-0, Wiley-VCH, Weinheim 2004
121. Schmidt, B. Larbig, G. ChemBioChem, 2004, 5,
122. Schmidt, B. ChemBioChem, 2004, 5, 1153-1154.
123. Schmidt, B. ChemBioChem, 2005, 6, 760-761
124. B. Schmidt, Proteins – Structure and Function, ChemBioChem, 2006, 7 (4), 702-703
125. B. Schmidt, The Adrenergic Receptors for the 21st Century, ChemMedChem, 2006, 1 (8), 904
126. S. Baumann, N. Höttecke, B. Schmidt, gamma-secretase as a target for AD, in Medicinal Chemistry of Alzheimer’s Disease, ed. A. Martinez, Research Signpost, 2008
127. N. Höttecke, S. Baumann, A. Taghavi, H.A. Braun, B. Schmidt, Drug Development and Diagnostics for Alzheimer's Disease Up to 2008, in: Frontiers in Medicinal Chemistry Vol. 4, Ed.: Atta-ur-Rahman, A.B. Reitz, 2009, pp. 730-766, Bentham Books 2009, ISBN 90-77527-07-9
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