Active Filters

  • (-) Journals = European Journal of Medicinal Chemistry
Search Results 1 - 20 of 33
Select Page
Synthesis of novel glutarimide ligands for the E3 ligase substrate receptor Cereblon (CRBN): Investigation of their binding mode and antiproliferative effects against myeloma cell lines
Krasavin, M., Adamchik, M., Bubyrev, A., Heim, C., Maiwald, S., Zhukovsky, D., … Hartmann, M. D. (2023). Synthesis of novel glutarimide ligands for the E3 ligase substrate receptor Cereblon (CRBN): Investigation of their binding mode and antiproliferative effects against myeloma cell lines. European Journal of Medicinal Chemistry, 246, 114990 (12 pp.). https://doi.org/10.1016/j.ejmech.2022.114990
Application of an “inhalation by design” approach to the identification and in-vitro evaluation of novel purine based PI3Kδ inhibitors
Mazzucato, R., Roberti, M., Capelli, A. M., Rancati, F., Biagetti, M., Fiorelli, C., … Pala, D. (2023). Application of an “inhalation by design” approach to the identification and in-vitro evaluation of novel purine based PI3Kδ inhibitors. European Journal of Medicinal Chemistry, 254, 115331 (15 pp.). https://doi.org/10.1016/j.ejmech.2023.115331
Tuning liver pyruvate kinase activity up or down with a new class of allosteric modulators
Nain-Perez, A., Nilsson, O., Lulla, A., Håversen, L., Brear, P., Liljenberg, S., … Grøtli, M. (2023). Tuning liver pyruvate kinase activity up or down with a new class of allosteric modulators. European Journal of Medicinal Chemistry, 250, 115177 (18 pp.). https://doi.org/10.1016/j.ejmech.2023.115177
Shifting the selectivity of pyrido[2,3-<em>d</em>]pyrimidin-7(8<em>H</em>)-one inhibitors towards the salt-inducible kinase (SIK) subfamily
Rak, M., Tesch, R., Berger, L. M., Shevchenko, E., Raab, M., Tjaden, A., … Knapp, S. (2023). Shifting the selectivity of pyrido[2,3-d]pyrimidin-7(8H)-one inhibitors towards the salt-inducible kinase (SIK) subfamily. European Journal of Medicinal Chemistry, 254, 115347. https://doi.org/10.1016/j.ejmech.2023.115347
Discovery of amino alcohols as highly potent, selective, and orally efficacious inhibitors of leukotriene A4 hydrolase
Thoma, G., Markert, C., Lueoend, R., Miltz, W., Spanka, C., Bollbuck, B., … Röhn, T. A. (2023). Discovery of amino alcohols as highly potent, selective, and orally efficacious inhibitors of leukotriene A4 hydrolase. European Journal of Medicinal Chemistry, 66, 16410-16425. https://doi.org/10.1021/acs.jmedchem.3c01866
A novel pan-selective bromodomain inhibitor for epigenetic drug design
Warstat, R., Pervaiz, M., Regenass, P., Amann, M., Schmidtkunz, K., Einsle, O., … Günther, S. (2023). A novel pan-selective bromodomain inhibitor for epigenetic drug design. European Journal of Medicinal Chemistry, 249, 115139 (12 pp.). https://doi.org/10.1016/j.ejmech.2023.115139
Development of [1,2]oxazoloisoindoles tubulin polymerization inhibitors: further chemical modifications and potential therapeutic effects against lymphomas
Barreca, M., Spanò, V., Rocca, R., Bivacqua, R., Abel, A. C., Maruca, A., … Barraja, P. (2022). Development of [1,2]oxazoloisoindoles tubulin polymerization inhibitors: further chemical modifications and potential therapeutic effects against lymphomas. European Journal of Medicinal Chemistry, 243, 114744 (25 pp.). https://doi.org/10.1016/j.ejmech.2022.114744
Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models
Menna, M., Fiorentino, F., Marrocco, B., Lucidi, A., Tomassi, S., Cilli, D., … Mai, A. (2022). Novel non-covalent LSD1 inhibitors endowed with anticancer effects in leukemia and solid tumor cellular models. European Journal of Medicinal Chemistry, 237, 114410 (23 pp.). https://doi.org/10.1016/j.ejmech.2022.114410
Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity
Zeinyeh, W., Esvan, Y. J., Josselin, B., Defois, M., Baratte, B., Knapp, S., … Moreau, P. (2022). Synthesis and biological evaluation of Haspin inhibitors: Kinase inhibitory potency and cellular activity. European Journal of Medicinal Chemistry, 236, 114369 (11 pp.). https://doi.org/10.1016/j.ejmech.2022.114369
Novel fragment-derived colchicine-site binders as microtubule-destabilizing agents
de la Roche, N. M., Mühlethaler, T., Di Martino, R. M. C., Ortega, J. A., Gioia, D., Roy, B., … Cavalli, A. (2022). Novel fragment-derived colchicine-site binders as microtubule-destabilizing agents. European Journal of Medicinal Chemistry, 241, 114614 (12 pp.). https://doi.org/10.1016/j.ejmech.2022.114614
Design, synthesis, biological evaluation and structural characterization of novel GEBR library PDE4D inhibitors
Brullo, C., Rapetti, F., Abbate, S., Prosdocimi, T., Torretta, A., Semrau, M., … Bruno, O. (2021). Design, synthesis, biological evaluation and structural characterization of novel GEBR library PDE4D inhibitors. European Journal of Medicinal Chemistry, 223, 113638 (13 pp.). https://doi.org/10.1016/j.ejmech.2021.113638
Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma
Jiang, B., Jiang, J., Kaltheuner, I. H., Iniguez, A. B., Anand, K., Ferguson, F. M., … Gray, N. S. (2021). Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma. European Journal of Medicinal Chemistry, 221, 113481 (16 pp.). https://doi.org/10.1016/j.ejmech.2021.113481
Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-<em>b</em>]pyridine core
Němec, V., Maier, L., Berger, B. T., Chaikuad, A., Drápela, S., Souček, K., … Paruch, K. (2021). Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core. European Journal of Medicinal Chemistry, 215, 113299 (8 pp.). https://doi.org/10.1016/j.ejmech.2021.113299
Structural basis for the design of bisubstrate inhibitors of protein kinase CK2 provided by complex structures with the substrate-competitive inhibitor heparin
Schnitzler, A., & Niefind, K. (2021). Structural basis for the design of bisubstrate inhibitors of protein kinase CK2 provided by complex structures with the substrate-competitive inhibitor heparin. European Journal of Medicinal Chemistry, 214, 113223 (9 pp.). https://doi.org/10.1016/j.ejmech.2021.113223
Does targeting Arg98 of FimH lead to high affinity antagonists?
Tomašič, T., Rabbani, S., Jakob, R. P., Reisner, A., Jakopin, Ž., Maier, T., … Anderluh, M. (2021). Does targeting Arg98 of FimH lead to high affinity antagonists? European Journal of Medicinal Chemistry, 211, 113093 (16 pp.). https://doi.org/10.1016/j.ejmech.2020.113093
Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor
Krämer, A., Kurz, C. G., Berger, B. T., Celik, I. E., Tjaden, A., Greco, F. A., … Hanke, T. (2020). Optimization of pyrazolo[1,5-a]pyrimidines lead to the identification of a highly selective casein kinase 2 inhibitor. European Journal of Medicinal Chemistry, 208, 112770 (17 pp.). https://doi.org/10.1016/j.ejmech.2020.112770
Selective targeting of the αC and DFG-out pocket in p38 MAPK
Röhm, S., Schröder, M., Dwyer, J. E., Widdowson, C. S., Chaikuad, A., Berger, B. T., … Knapp, S. (2020). Selective targeting of the αC and DFG-out pocket in p38 MAPK. European Journal of Medicinal Chemistry, 208, 112721 (35 pp.). https://doi.org/10.1016/j.ejmech.2020.112721
Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents
Brindisi, M., Ulivieri, C., Alfano, G., Gemma, S., de Asís Balaguer, F., Khan, T., … Brogi, S. (2019). Structure-activity relationships, biological evaluation and structural studies of novel pyrrolonaphthoxazepines as antitumor agents. European Journal of Medicinal Chemistry, 162, 290-320. https://doi.org/10.1016/j.ejmech.2018.11.004
Lead optimization and biological evaluation of fragment-based cN-II inhibitors
Guillon, R., Rahimova, R., Preeti, P., Egron, D., Rouanet, S., Dumontet, C., … Peyrottes, S. (2019). Lead optimization and biological evaluation of fragment-based cN-II inhibitors. European Journal of Medicinal Chemistry, 168, 28-44. https://doi.org/10.1016/j.ejmech.2019.02.040
Development of alkyl glycerone phosphate synthase inhibitors: structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells
Stazi, G., Battistelli, C., Piano, V., Mazzone, R., Marrocco, B., Marchese, S., … Valente, S. (2019). Development of alkyl glycerone phosphate synthase inhibitors: structure-activity relationship and effects on ether lipids and epithelial-mesenchymal transition in cancer cells. European Journal of Medicinal Chemistry, 163, 722-735. https://doi.org/10.1016/j.ejmech.2018.11.050