Grädler U - Search Results

1

Structure-based optimization of non-peptidic Cathepsin D inhibitors.

Grädler U, Czodrowski P, Tsaklakidis C, Klein M, Werkmann D, Lindemann S, Maskos K, Leuthner B. Grädler U, et al. Bioorg Med Chem Lett. 2014 Sep 1;24(17):4141-50. doi: 10.1016/j.bmcl.2014.07.054. Epub 2014 Jul 25. Bioorg Med Chem Lett. 2014. PMID: 25086681

2

Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.

Grädler U, Fuchss T, Ulrich WR, Boer R, Strub A, Hesslinger C, Anézo C, Diederichs K, Zaliani A. Grädler U, et al. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4228-32. doi: 10.1016/j.bmcl.2011.05.073. Epub 2011 May 30. Bioorg Med Chem Lett. 2011. PMID: 21684157

3

Fragment-based discovery of hydroxy-indazole-carboxamides as novel small molecule inhibitors of Hsp90.

Buchstaller HP, Eggenweiler HM, Sirrenberg C, Grädler U, Musil D, Hoppe E, Zimmermann A, Schwartz H, März J, Bomke J, Wegener A, Wolf M. Buchstaller HP, et al. Among authors: gradler u. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4396-403. doi: 10.1016/j.bmcl.2012.04.121. Epub 2012 May 5. Bioorg Med Chem Lett. 2012. PMID: 22632933

4

Fragment-based discovery of new highly substituted 1H-pyrrolo[2,3-b]- and 3H-imidazolo[4,5-b]-pyridines as focal adhesion kinase inhibitors.

Heinrich T, Seenisamy J, Emmanuvel L, Kulkarni SS, Bomke J, Rohdich F, Greiner H, Esdar C, Krier M, Grädler U, Musil D. Heinrich T, et al. Among authors: gradler u. J Med Chem. 2013 Feb 14;56(3):1160-70. doi: 10.1021/jm3016014. Epub 2013 Jan 22. J Med Chem. 2013. PMID: 23294348

5

Fragment-based discovery of focal adhesion kinase inhibitors.

Grädler U, Bomke J, Musil D, Dresing V, Lehmann M, Hölzemann G, Greiner H, Esdar C, Krier M, Heinrich T. Grädler U, et al. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5401-9. doi: 10.1016/j.bmcl.2013.07.050. Epub 2013 Jul 31. Bioorg Med Chem Lett. 2013. PMID: 23973211

6

Allosteric IGF-1R Inhibitors.

Heinrich T, Grädler U, Böttcher H, Blaukat A, Shutes A. Heinrich T, et al. Among authors: gradler u. ACS Med Chem Lett. 2010 May 18;1(5):199-203. doi: 10.1021/ml100044h. eCollection 2010 Aug 12. ACS Med Chem Lett. 2010. PMID: 24900194 Free PMC article.

7

Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.

Dorsch D, Schadt O, Stieber F, Meyring M, Grädler U, Bladt F, Friese-Hamim M, Knühl C, Pehl U, Blaukat A. Dorsch D, et al. Among authors: gradler u. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1597-602. doi: 10.1016/j.bmcl.2015.02.002. Epub 2015 Feb 16. Bioorg Med Chem Lett. 2015. PMID: 25736998

8

Discovery of novel 7-azaindoles as PDK1 inhibitors.

Wucherer-Plietker M, Merkul E, Müller TJJ, Esdar C, Knöchel T, Heinrich T, Buchstaller HP, Greiner H, Dorsch D, Finsinger D, Calderini M, Bruge D, Grädler U. Wucherer-Plietker M, et al. Among authors: gradler u. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3073-3080. doi: 10.1016/j.bmcl.2016.05.005. Epub 2016 May 4. Bioorg Med Chem Lett. 2016. PMID: 27217002

9

Ligand Desolvation Steers On-Rate and Impacts Drug Residence Time of Heat Shock Protein 90 (Hsp90) Inhibitors.

Schuetz DA, Richter L, Amaral M, Grandits M, Grädler U, Musil D, Buchstaller HP, Eggenweiler HM, Frech M, Ecker GF. Schuetz DA, et al. Among authors: gradler u. J Med Chem. 2018 May 24;61(10):4397-4411. doi: 10.1021/acs.jmedchem.8b00080. Epub 2018 May 10. J Med Chem. 2018. PMID: 29701469

10

Discovery of novel Cyclophilin D inhibitors starting from three dimensional fragments with millimolar potencies.

Grädler U, Schwarz D, Blaesse M, Leuthner B, Johnson TL, Bernard F, Jiang X, Marx A, Gilardone M, Lemoine H, Roche D, Jorand-Lebrun C. Grädler U, et al. Bioorg Med Chem Lett. 2019 Dec 1;29(23):126717. doi: 10.1016/j.bmcl.2019.126717. Epub 2019 Oct 16. Bioorg Med Chem Lett. 2019. PMID: 31635932 Free PMC article.

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