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2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.
Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R, Schwarz D, Musil D, Burke R, Urbahns K, Workman P, Wienke D, Clarke PA, Raynaud FI, Eccles SA, Esdar C, Rohdich F, Blagg J. Mallinger A, et al. Among authors: urbahns k. ACS Med Chem Lett. 2016 Mar 28;7(6):573-8. doi: 10.1021/acsmedchemlett.6b00022. eCollection 2016 Jun 9. ACS Med Chem Lett. 2016. PMID: 27326329 Free PMC article.
Discovery of potent and selective CDK8 inhibitors from an HSP90 pharmacophore.
Schiemann K, Mallinger A, Wienke D, Esdar C, Poeschke O, Busch M, Rohdich F, Eccles SA, Schneider R, Raynaud FI, Czodrowski P, Musil D, Schwarz D, Urbahns K, Blagg J. Schiemann K, et al. Among authors: urbahns k. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1443-51. doi: 10.1016/j.bmcl.2016.01.062. Epub 2016 Jan 22. Bioorg Med Chem Lett. 2016. PMID: 26852363
Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening.
Czodrowski P, Mallinger A, Wienke D, Esdar C, Pöschke O, Busch M, Rohdich F, Eccles SA, Ortiz-Ruiz MJ, Schneider R, Raynaud FI, Clarke PA, Musil D, Schwarz D, Dale T, Urbahns K, Blagg J, Schiemann K. Czodrowski P, et al. Among authors: urbahns k. J Med Chem. 2016 Oct 27;59(20):9337-9349. doi: 10.1021/acs.jmedchem.6b00597. Epub 2016 Oct 7. J Med Chem. 2016. PMID: 27490956 Free article.
Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases.
Clarke PA, Ortiz-Ruiz MJ, TePoele R, Adeniji-Popoola O, Box G, Court W, Czasch S, El Bawab S, Esdar C, Ewan K, Gowan S, De Haven Brandon A, Hewitt P, Hobbs SM, Kaufmann W, Mallinger A, Raynaud F, Roe T, Rohdich F, Schiemann K, Simon S, Schneider R, Valenti M, Weigt S, Blagg J, Blaukat A, Dale TC, Eccles SA, Hecht S, Urbahns K, Workman P, Wienke D. Clarke PA, et al. Among authors: urbahns k. Elife. 2016 Dec 9;5:e20722. doi: 10.7554/eLife.20722. Elife. 2016. PMID: 27935476 Free PMC article.
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L. Caldwell RD, et al. Among authors: urbahns k. J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15. J Med Chem. 2019. PMID: 31368705
Small molecules-Giant leaps for immuno-oncology.
Kötzner L, Huck B, Garg S, Urbahns K. Kötzner L, et al. Among authors: urbahns k. Prog Med Chem. 2020;59:1-62. doi: 10.1016/bs.pmch.2019.11.001. Epub 2020 Jan 20. Prog Med Chem. 2020. PMID: 32362326 Review.
Targeted Covalent Inhibitors for the Treatment of Malaria?
Kulkarni S, Urbahns K, Spangenberg T. Kulkarni S, et al. Among authors: urbahns k. ACS Infect Dis. 2020 Nov 13;6(11):2815-2817. doi: 10.1021/acsinfecdis.0c00684. Epub 2020 Oct 15. ACS Infect Dis. 2020. PMID: 33054158
Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides.
Urbahns K, Härter M, Albers M, Schmidt D, Stelte-Ludwig B, Brüggemeier U, Vaupel A, Keldenich J, Lustig K, Tsujishita H, Gerdes C. Urbahns K, et al. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6151-4. doi: 10.1016/j.bmcl.2007.09.039. Epub 2007 Sep 14. Bioorg Med Chem Lett. 2007. PMID: 17910915
Tetrahydro-naphthols as orally available TRPV1 inhibitors.
Urbahns K, Yura T, Gupta JB, Tajimi M, Fujishima H, Masuda T, Yamamoto N, Ikegami Y, Marumo M, Yasoshima K, Yoshida N, Moriwaki T, Madge D, Chan F, Mogi M. Urbahns K, et al. Bioorg Med Chem Lett. 2012 May 15;22(10):3408-11. doi: 10.1016/j.bmcl.2012.03.108. Epub 2012 Apr 6. Bioorg Med Chem Lett. 2012. PMID: 22525313
28 results