Medicinal Chemistry

  • 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.