Drug Design

Organisational unit: Research Group

  1. 2017
  2. Zak, K. M., Grudnik, P., Magiera, K., Dömling, A., Dubin, G., & Holak, T. A. (2017). Structural Biology of the Immune Checkpoint Receptor PD-1 and Its Ligands PD-L1/PD-L2. Structure, 25(8), 1163-1174. DOI: 10.1016/j.str.2017.06.011
  3. Twarda-Clapa, A., Krzanik, S., Kubica, K., Guzik, K., Labuzek, B., Neochoritis, C. G., ... Holak, T. A. (2017). 1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers. Journal of Medicinal Chemistry, 60(10), 4234-4244. DOI: 10.1021/acs.jmedchem.7b00104
  4. Shaabani, S., Neochoritis, C. G., Twarda-Clapa, A., Musielak, B., Holak, T. A., & Domling, A. (2017). Scaffold hopping via ANCHOR.QUERY: beta-lactams as potent p53-MDM2 antagonists. MedChemCommun, 8(5), 1046-1052. DOI: 10.1039/c7md00058h
  5. Kroon, E. (2017). Exploring multicomponent reactions: From chemistry to drug design [Groningen]: Rijksuniversiteit Groningen
  6. Zarganes Tzitzikas, T. (2017). Innovative multicomponent reactions and their use in medicinal chemistry [Groningen]: University of Groningen
  7. Chandgude, A. (2017). Multicomponent reactions: development, scope, and applications [Groningen]: University of Groningen
  8. 2016
  9. Surmiak, E., Twarda-Clapa, A., Zak, K. M., Musielak, B., Tomala, M. D., Kubica, K., ... Holak, T. A. (2016). A Unique Mdm2-Binding Mode of the 3-Pyrrolin-2-one- and 2-Furanone-Based Antagonists of the p53-Mdm2 Interaction. ACS chemical biology, 11(12), 3310-3318. DOI: 10.1021/acschembio.6b00596
  10. Livadiotou, D., Hatzimimikou, D., Tsitsi, D., Tsiaras, V., Samatidou, E., & Neochoritis, C. (2016). One-pot reaction of pyranoindolones with phenylisocyanates: a simple and regioselective approach to b-carbolines. Tetrahedron Letters, 57(49), 5453-5456. DOI: 10.1016/j.tetlet.2016.10.075
  11. Fuggetta, M. P., De Mico, A., Cottarelli, A., Morelli, F., Zonfrillo, M., Ulgheri, F., ... Spanu, P. (2016). Synthesis and Enantiomeric Separation of a Novel Spiroketal Derivative: A Potent Human Telomerase Inhibitor with High in Vitro Anticancer Activity. Journal of Medicinal Chemistry, 59(19), 9140-9149. DOI: 10.1021/acs.jmedchem.6b01046
  12. Zak, K. M., Grudnik, P., Guzik, K., Zieba, B. J., Musielak, B., Dömling, A., ... Holak, T. A. (2016). Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1). Oncotarget, 7(21), 30323-30335. DOI: 10.18632/oncotarget.8730
  13. Boltjes, A., Shrinidhi, A., van de Kolk, K., Herdtweck, E., & Dömling, A. (2016). Gd-TEMDO: Design, Synthesis, and MRI Application. Chemistry, 22(22), 7352-7356. DOI: 10.1002/chem.201600720
  14. Patil, P., Zhang, J., Kurpiewska, K., Kalinowska-Tłuścik, J., & Dömling, A. (2016). Hydrazine in the Ugi Tetrazole Reaction. Synthesis, 48(8), 1122-1130. DOI: 10.1055/s-0035-1561353
  15. Zhao, T., Kurpiewska, K., Kalinowska-Tłuścik, J., Herdtweck, E., & Dömling, A. (2016). α-Amino Acid-Isosteric α-Amino Tetrazoles. Chemistry, 22(9), 3009-3018. DOI: 10.1002/chem.201504520
  16. Kroon, E., Kurpiewska, K., Kalinowska-Tłuścik, J., & Dömling, A. (2016). Cleavable β-Cyanoethyl Isocyanide in the Ugi Tetrazole Reaction. Organic letters, 18(19), 4762-4765. DOI: 10.1021/acs.orglett.6b01826
  17. Zhao, T. (2016). Novel Applications of Tetrazoles Derived from the TMSN3-Ugi Reaction [Groningen]: Rijksuniversiteit Groningen
  18. Neochoritis, C., Livadiotou, D., Tsiaras, V., Zarganes Tzitzikas, T., & Samatidou, E. (2016). The indoleacetic acids in IMCRs: a three-component Ugi reaction involving TosMIC. Tetrahedron, 72(33), 5149-5156. DOI: 10.1016/j.tet.2016.07.013
  19. 2015
  20. Zak, K. M., Kitel, R., Przetocka, S., Golik, P., Guzik, K., Musielak, B., ... Holak, T. A. (2015). Structure of the Complex of Human Programmed Death 1, PD-1, and Its Ligand PD-L1. Structure, 23(12), 2341-2348. DOI: 10.1016/j.str.2015.09.010
  21. Giewekemeyer, K., Hackenberger, C., Aquila, A., Wilke, R. N., Groves, M., Jordanova, R., ... Mancuso, A. P. (2015). Tomography of a Cryo-immobilized Yeast Cell Using Ptychographic Coherent X-Ray Diffractive Imaging. Biophysical Journal, 109(9), 1986-1995. DOI: 10.1016/j.bpj.2015.08.047
  22. Wu, S., Huang, J., Gazzarrini, S., He, S., Chen, L., Li, J., ... Wang, W. (2015). Isocyanides as Influenza A Virus Subtype H5N1 Wild-Type M2 Channel Inhibitors. ChemMedChem, 10(11), 1837-45. DOI: 10.1002/cmdc.201500318
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