Medicinal Chemistry

  • Beta-Thalassemia Minor and SARS-CoV-2: Physiopathology, Prevalence, Severity, Morbidity, and Mortality
    E. Lansiaux, E. Drouin, C. Bolm, Thalass. Rep. 2023, 13, 21–32.
    Also published as a preprint at medRxiv.

  • PARP targeted Auger emitter therapy with [125I]PARPi-01 for triple-negative breast cancer
    R. Ambur Sankaranarayana, A. Florea, S. Allekotte, A. T. J. Vogg, J. Maurer, L. Schäfer, C. Bolm, S. Terhorst, A. Classen, M. Bauwens, A. Morgenroth, F. M. Mottaghy, EJNMMI Res. 2022, 12, 60.

  • Preparation of Enantiopure 3-Aminopiperidine and 3-Aminoazepane Derivatives from Ornithine and Lysine. Consecutive Syntheses of Pharmacologically Active Analogs, Such as Besifloxacin
    I. Schiffers, M. Frings, B. M. Kübber, K.-N. Truong, K. Rissanen, C. Bolm, Org. Process Res. Dev. 2022, 26, 2811–2822.
    Watch the video to see how (S)-3-(tritylamino)piperidin-2-one, an intermediate product from this publication, is purified by manual grinding.

  • Auger Emitter Conjugated PARP Inhibitor for Therapy in Triple Negative Breast Cancers: A Comparative In-Vitro Study
    A. Sankaranarayanan, J. Peil, A. T. J. Vogg, C. Bolm, S. Terhorst, A. Classen, M. Bauwens, J. Maurer, F. Mottaghy, A. Morgenroth, Cancers 2022, 14, 230.

  • New Kids on the Block: Bile Salt Conjugates of Microbial Origin
    Ü. Ay, M. Leníček, A. Classen, S. W. M. Olde Damink, C. Bolm, F. G. Schaap, Metabolites 2022, 12, 176.

  • Evaluation of 3- and 4-Phenoxybenzamides as Selective Inhibitors of the Mono-ADP-Ribosyltransferase PARP10
    P. Korn, A. Classen, S. Murthy, R. Guareschi, M. M. Maksimainen, B. E. Lippok, A. Galera-Prat, S. T. Sowa, C. Voigt, G. Rossetti, L. Lehtiö, C. Bolm, B. Lüscher, ChemistryOpen 2021, 10, 939–948.

  • Bromodomain Inhibitors
    C. Bolm, M. Frings, J.-H. Schöbel, N. Chatain, B. Altenburg, G. Rossetti, J. Gossen, S. Koschmieder, Patent application, WO2021083879 (A1), May 06, 2021.
    For additional information, please see here.

  • NH-sulfoximine: A novel pharmacological inhibitor of the mitochondrial F1Fo‐ATPase, which suppresses viability of cancerous cells
    D. Strobbe, R. Pecorari, O. Conte, A. Minutolo, C. M. M. Hendriks, S. Wiezorek, D. Faccenda, R. Abeti, C. Montesano, C. Bolm, M. Campanella, Br. J. Pharmacol. 2021, 178, 298–311.

  • The Sulfilimine Analogue of Allicin, S-Allyl-S-(S-allyl)-N-Cyanosulfilimine, Is Antimicrobial and Reacts with Glutathione
    T. Horn, W. Bettray, U. Noll, F. Krauskopf, M.-R. Huang, C. Bolm, A. J. Slusarenko, M. C. H. Gruhlke, Antioxidants 2020, 9, 1086.

  • The mono-ADP-ribosyltransferase ARTD10 regulates the voltage-gated K+ channel Kv1.1 through protein kinase C delta
    Y. Tian, P. Korn, P. Tripathi, D. Komnig, D. Wiemuth, A. Nikouee, A. Classen, C. Bolm, B. H. Falkenburger, B. Lüscher, S. Gründer, BMC Biol. 2020, 18, 143.

  • Chiral Analogues of PFI-1 as BET Inhibitors and Their Functional Role in Myeloid Malignancies
    B. Altenburg, M. Frings, J.-H. Schöbel, J. Goßen, K. Pannen, K. Vanderliek, G. Rossetti, S. Koschmieder, N. Chatain, C. Bolm, ACS Med. Chem. Lett. 2020, 11, 1928–1934. Part of the special issue “Medicinal Chemistry: From Targets to Therapies”.

  • Novel Broccoli Sulforaphane-Based Analogues Inhibit the Progression of Pancreatic Cancer without Side Effects
    C. Georgikou, L. Buglioni, M. Bremerich, N. Roubicek, L. Yin, W. Gross, C. Sticht, C. Bolm, I. Herr, Biomolecules 2020, 10, 769.

  • Inhibitoren für Bromodomänen
    M. Frings, J.-H. Schoebel, B. Altenburg, N. Chatain, S. Koschmieder, G. Rossetti, J. Gossen, C. Bolm, Patentanmeldung, Anmeldenummer DE 10 2019 129 527.0, October 31, 2019.

  • Sulforaphane Modifies Histone H3, Unpacks Chromatin, and Primes Defense
    B. Schillheim, I. Jansen, S. Baum, A. Beesley, C. Bolm, U. Conrath, Plant Physiol. 2018, 176, 2395–2405.

  • New ATR inhibitors for the use in cancer therapy
    C. Bolm, C. M. M. Hendriks, B. Lüscher, J. Hartkamp, WO application 2018029117, February 15, 2018.

  • Anti-glioma Activity of Dapsone and Its Enhancement by Synthetic Chemical Modification
    G. Karpel-Massler, R. E. Kast, M. D. Siegelin, A. Dwucet, E. Schneider, M.-A. Westhoff, C. R. Wirtz, X. Y. Chen, M.-E. Halatsch, C. Bolm, Neurochem. Res. 2017, 42, 3382–3389.

  • Sulfoximines as ATR inhibitors: Analogs of VE-821
    C. M. M. Hendriks, J. Hartkamp, S. Wiezorek, A.-D. Steinkamp, G. Rossetti, B. Lüscher, C. Bolm, Bioorg. Med. Chem. Lett. 2017, 27, 2659–2662.

  • Sulfoximines from a Medicinal Chemist’s Perspective: Physicochemical and in vitro Parameters Relevant for Drug Discovery
    M. Frings, C. Bolm, A. Blum, C. Gnamm, Eur. J. Med. Chem. 2017, 126, 225–245.

  • Synthesis of a sulfonimidamide-based analog of Tasisulam and its biological evaluation in the melanoma cell lines SKMel23 and A375
    A.-D. Steinkamp, L. Schmitt, X. Chen, K. Fietkau, R. Heise, J. Baron, C. Bolm, Skin Pharmacol. Physiol. 2016, 29, 281–290.

  • Synthesis of N-Cyano-substituted Sulfilimine and Sulfoximine Derivatives of S0859 and their Biological Evaluation as Sodium Bicarbonate Co-transport Inhibitors
    A.-D. Steinkamp, N. Seling, S. Lee, E. Boedtkjer, C. Bolm, MedChemCommun 2015, 6, 2163–2169.

  • Pentafluorosulfanyl-containing flufenamic acid analogs: Syntheses, properties and biological activities
    C. M. M. Hendriks, T. M. Penning, T. Zang, D. Wiemuth, S. Gründer, I. A. Sanhueza, F. Schoenebeck, C. Bolm, Bioorg. Med. Chem. Lett. 2015, 25, 4437–4440.

  • Methionine and Buthionine Sulfoximine: Syntheses under Mild and Safe Imidation/Oxidation Conditions
    L. Buglioni, V. Bizet, C. Bolm, Adv. Synth. Catal. 2014, 356, 2209–2213.

  • N-Cyano Sulfoximines: COX Inhibition, anti-Cancer Activity, Cellular Toxicity, and Mutagenicity 
    S. J. Park, H. Baars, H. Buschmann, J. M. Baron, P. M. Amann, K. Czaja, H. Hollert, K. Bluhm, R. Redelstein, C. Bolm, ChemMedChem. 2013, 8, 217–220.

  • Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins
    X. Y. Chen, S. J. Park, H. Buschmann, M. De Rosa, C. Bolm, Bioorg. Med. Chem. Lett. 2012, 22, 4307–4309.

  • Bioactive Sulfoximines: Syntheses and properties of Vioxx® analogs
    S. J. Park, H. Buschmann, C. Bolm, Bioorg. Med. Chem. Lett. 2011, 21, 4888–4890.