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Page 1
Discovery of a novel class of highly potent inhibitors of the p53-MDM2 interaction by structure-based design starting from a conformational argument.
Furet P, Masuya K, Kallen J, Stachyra-Valat T, Ruetz S, Guagnano V, Holzer P, Mah R, Stutz S, Vaupel A, Chène P, Jeay S, Schlapbach A. Furet P, et al. Among authors: schlapbach a. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4837-4841. doi: 10.1016/j.bmcl.2016.08.010. Epub 2016 Aug 9. Bioorg Med Chem Lett. 2016. PMID: 27542305
In vitro and in vivo characterization of a novel, highly potent p53-MDM2 inhibitor.
Vaupel A, Holzer P, Ferretti S, Guagnano V, Kallen J, Mah R, Masuya K, Ruetz S, Rynn C, Schlapbach A, Stachyra T, Stutz S, Todorov M, Jeay S, Furet P. Vaupel A, et al. Among authors: schlapbach a. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3404-3408. doi: 10.1016/j.bmcl.2018.08.027. Epub 2018 Aug 26. Bioorg Med Chem Lett. 2018. PMID: 30217415
Structural States of Hdm2 and HdmX: X-ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes.
Kallen J, Izaac A, Chau S, Wirth E, Schoepfer J, Mah R, Schlapbach A, Stutz S, Vaupel A, Guagnano V, Masuya K, Stachyra TM, Salem B, Chene P, Gessier F, Holzer P, Furet P. Kallen J, et al. Among authors: schlapbach a. ChemMedChem. 2019 Jul 17;14(14):1305-1314. doi: 10.1002/cmdc.201900201. Epub 2019 May 27. ChemMedChem. 2019. PMID: 31066983
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
Velcicky J, Feifel R, Hawtin S, Heng R, Huppertz C, Koch G, Kroemer M, Moebitz H, Revesz L, Scheufler C, Schlapbach A. Velcicky J, et al. Among authors: schlapbach a. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1293-7. doi: 10.1016/j.bmcl.2009.10.138. Epub 2009 Nov 3. Bioorg Med Chem Lett. 2010. PMID: 20060294
N-aryl-piperidine-4-carboxamides as a novel class of potent inhibitors of MALT1 proteolytic activity.
Schlapbach A, Revesz L, Pissot Soldermann C, Zoller T, Régnier CH, Bornancin F, Radimerski T, Blank J, Schuffenhauer A, Renatus M, Erbel P, Melkko S, Heng R, Simic O, Endres R, Wartmann M, Quancard J. Schlapbach A, et al. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2153-2158. doi: 10.1016/j.bmcl.2018.05.017. Epub 2018 May 9. Bioorg Med Chem Lett. 2018. PMID: 29759726
Design and preparation of 2-benzamido-pyrimidines as inhibitors of IKK.
Waelchli R, Bollbuck B, Bruns C, Buhl T, Eder J, Feifel R, Hersperger R, Janser P, Revesz L, Zerwes HG, Schlapbach A. Waelchli R, et al. Among authors: schlapbach a. Bioorg Med Chem Lett. 2006 Jan 1;16(1):108-12. doi: 10.1016/j.bmcl.2005.09.035. Epub 2005 Oct 19. Bioorg Med Chem Lett. 2006. PMID: 16236504
Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Velcicky J, Wilcken R, Cotesta S, Janser P, Schlapbach A, Wagner T, Piechon P, Villard F, Bouhelal R, Piller F, Harlfinger S, Stringer R, Fehlmann D, Kaupmann K, Littlewood-Evans A, Haffke M, Gommermann N. Velcicky J, et al. Among authors: schlapbach a. J Med Chem. 2020 Sep 10;63(17):9856-9875. doi: 10.1021/acs.jmedchem.0c01020. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32856916
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part II.
Revesz L, Schlapbach A, Aichholz R, Dawson J, Feifel R, Hawtin S, Littlewood-Evans A, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C. Revesz L, et al. Among authors: schlapbach a. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4719-23. doi: 10.1016/j.bmcl.2010.04.023. Epub 2010 Apr 11. Bioorg Med Chem Lett. 2010. PMID: 20591669
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.
Revesz L, Schlapbach A, Aichholz R, Feifel R, Hawtin S, Heng R, Hiestand P, Jahnke W, Koch G, Kroemer M, Möbitz H, Scheufler C, Velcicky J, Huppertz C. Revesz L, et al. Among authors: schlapbach a. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4715-8. doi: 10.1016/j.bmcl.2010.04.024. Epub 2010 Apr 13. Bioorg Med Chem Lett. 2010. PMID: 20594847
23 results