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Page 1
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: scheufler c. 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
Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity.
Schlapbach A, Feifel R, Hawtin S, Heng R, Koch G, Moebitz H, Revesz L, Scheufler C, Velcicky J, Waelchli R, Huppertz C. Schlapbach A, et al. Among authors: scheufler c. Bioorg Med Chem Lett. 2008 Dec 1;18(23):6142-6. doi: 10.1016/j.bmcl.2008.10.039. Epub 2008 Oct 11. Bioorg Med Chem Lett. 2008. PMID: 18945615
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: scheufler c. 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: scheufler c. 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
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Chen C, Zhu H, Stauffer F, Caravatti G, Vollmer S, Machauer R, Holzer P, Möbitz H, Scheufler C, Klumpp M, Tiedt R, Beyer KS, Calkins K, Guthy D, Kiffe M, Zhang J, Gaul C. Chen C, et al. Among authors: scheufler c. ACS Med Chem Lett. 2016 Jun 1;7(8):735-40. doi: 10.1021/acsmedchemlett.6b00167. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563395 Free PMC article.
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach.
Möbitz H, Machauer R, Holzer P, Vaupel A, Stauffer F, Ragot C, Caravatti G, Scheufler C, Fernandez C, Hommel U, Tiedt R, Beyer KS, Chen C, Zhu H, Gaul C. Möbitz H, et al. Among authors: scheufler c. ACS Med Chem Lett. 2017 Feb 14;8(3):338-343. doi: 10.1021/acsmedchemlett.6b00519. eCollection 2017 Mar 9. ACS Med Chem Lett. 2017. PMID: 28337327 Free PMC article.
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Smith A, Ni ZJ, Poon D, Huang Z, Chen Z, Zhang Q, Tandeske L, Merritt H, Shoemaker K, Chan J, Kaufman S, Huh K, Murray J, Appleton BA, Cowan-Jacob SW, Scheufler C, Kanazawa T, Jansen JM, Stuart D, Shafer CM. Smith A, et al. Among authors: scheufler c. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5221-5224. doi: 10.1016/j.bmcl.2017.10.047. Epub 2017 Oct 20. Bioorg Med Chem Lett. 2017. PMID: 29107542
Identification of TAK-756, A Potent TAK1 Inhibitor for the Treatment of Osteoarthritis through Intra-Articular Administration.
Langlois JB, Brenneisen S, Rodde S, Vangrevelinghe E, Rose G, Lerch P, Sorge M, Ullrich T, Patora-Komisarska K, Quancard J, Larger P, Gianola L, Textor C, Chenal G, Rubic-Schneider T, Simkova K, Masmanidou O, Scheufler C, Lammens A, Bouzan A, Demirci S, Flotte L, Rivet H, Hartmann L, Guezel D, Flueckiger M, Schilb A, Schuepbach E, Kettle R, Jacobi C, Pearson D, Richards PJ, Minetti GC. Langlois JB, et al. Among authors: scheufler c. J Med Chem. 2024 Dec 12;67(23):21163-21185. doi: 10.1021/acs.jmedchem.4c01938. Epub 2024 Nov 22. J Med Chem. 2024. PMID: 39576936
Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent.
Andraos R, Qian Z, Bonenfant D, Rubert J, Vangrevelinghe E, Scheufler C, Marque F, Régnier CH, De Pover A, Ryckelynck H, Bhagwat N, Koppikar P, Goel A, Wyder L, Tavares G, Baffert F, Pissot-Soldermann C, Manley PW, Gaul C, Voshol H, Levine RL, Sellers WR, Hofmann F, Radimerski T. Andraos R, et al. Among authors: scheufler c. Cancer Discov. 2012 Jun;2(6):512-523. doi: 10.1158/2159-8290.CD-11-0324. Epub 2012 May 3. Cancer Discov. 2012. PMID: 22684457 Free PMC article.
40 results