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Items: 1 to 20 of 43

1.

Novel Protein Kinase Inhibitors Related to Tau Pathology Modulate Tau Protein-Self Interaction Using a Luciferase Complementation Assay.

Holzer M, Schade N, Opitz A, Hilbrich I, Stieler J, Vogel T, Neukel V, Oberstadt M, Totzke F, Schächtele C, Sippl W, Hilgeroth A.

Molecules. 2018 Sep 12;23(9). pii: E2335. doi: 10.3390/molecules23092335.

2.

Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and PDGFR-β related to anticancer drug resistance.

Fischer T, Najjar K, Totzke F, Schächtele C, Sippl W, Ritter C, Hilgeroth A.

J Enzyme Inhib Med Chem. 2018 Dec;33(1):1-8. doi: 10.1080/14756366.2017.1370583.

3.

Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors.

Fischer T, Krüger T, Najjar A, Totzke F, Schächtele C, Sippl W, Ritter C, Hilgeroth A.

Bioorg Med Chem Lett. 2017 Jun 15;27(12):2708-2712. doi: 10.1016/j.bmcl.2017.04.053. Epub 2017 Apr 19.

PMID:
28478927
4.

Scaffold hopping identifies 6,8-disubstituted purines as novel anaplastic lymphoma kinase inhibitors.

Schlütke L, Immer M, Preu L, Totzke F, Schächtele C, Kubbutat MHG, Kunick C.

Eur J Pharm Biopharm. 2018 May;126:89-94. doi: 10.1016/j.ejpb.2017.03.011. Epub 2017 Mar 15.

PMID:
28315448
5.

Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and IGF-1R.

Hempel C, Totzke F, Schächtele C, Najjar A, Sippl W, Ritter C, Hilgeroth A.

J Enzyme Inhib Med Chem. 2017 Dec;32(1):271-276. doi: 10.1080/14756366.2016.1247062.

6.

Drug Development of Small-Molecule Inhibitors of AD-Relevant Kinases as Novel Perspective Multitargeted Approach.

Tell V, Hilbrich I, Holzer M, Totzke F, Schachtele C, Slynko I, Sippl W, Hilgeroth A.

Curr Alzheimer Res. 2016;13(12):1330-1336. Review.

PMID:
27306698
7.

Optimization of potent DFG-in inhibitors of platelet derived growth factor receptorβ (PDGF-Rβ) guided by water thermodynamics.

Horbert R, Pinchuk B, Johannes E, Schlosser J, Schmidt D, Cappel D, Totzke F, Schächtele C, Peifer C.

J Med Chem. 2015 Jan 8;58(1):170-82. doi: 10.1021/jm500373x. Epub 2014 Jul 21.

PMID:
25007344
8.

Development of first lead structures for phosphoinositide 3-kinase-C2γ inhibitors.

Freitag A, Prajwal P, Shymanets A, Harteneck C, Nürnberg B, Schächtele C, Kubbutat M, Totzke F, Laufer SA.

J Med Chem. 2015 Jan 8;58(1):212-21. doi: 10.1021/jm5006034. Epub 2014 Jul 14.

PMID:
24983663
9.

Discovery of 4-anilino α-carbolines as novel Brk inhibitors.

Mahmoud KA, Krug M, Wersig T, Slynko I, Schächtele C, Totzke F, Sippl W, Hilgeroth A.

Bioorg Med Chem Lett. 2014 Apr 15;24(8):1948-51. doi: 10.1016/j.bmcl.2014.03.002. Epub 2014 Mar 12.

PMID:
24650640
10.

Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors.

Barbosa ML, Lima LM, Tesch R, Sant'Anna CM, Totzke F, Kubbutat MH, Schächtele C, Laufer SA, Barreiro EJ.

Eur J Med Chem. 2014 Jan;71:1-14. doi: 10.1016/j.ejmech.2013.10.058. Epub 2013 Oct 31.

PMID:
24269511
12.

Assessing the target differentiation potential of imidazole-based protein kinase inhibitors.

Dimova D, Iyer P, Vogt M, Totzke F, Kubbutat MH, Schächtele C, Laufer S, Bajorath J.

J Med Chem. 2012 Dec 27;55(24):11067-71. doi: 10.1021/jm3014508. Epub 2012 Dec 11.

PMID:
23210446
13.

Multitargeted drug development: Discovery and profiling of dihydroxy substituted 1-aza-9-oxafluorenes as lead compounds targeting Alzheimer disease relevant kinases.

Tell V, Holzer M, Herrmann L, Mahmoud KA, Schächtele C, Totzke F, Hilgeroth A.

Bioorg Med Chem Lett. 2012 Nov 15;22(22):6914-8. doi: 10.1016/j.bmcl.2012.09.006. Epub 2012 Sep 13.

PMID:
23039927
14.

2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.

Determann R, Dreher J, Baumann K, Preu L, Jones PG, Totzke F, Schächtele C, Kubbutat MH, Kunick C.

Eur J Med Chem. 2012 Jul;53:254-63. doi: 10.1016/j.ejmech.2012.04.007. Epub 2012 Apr 14.

PMID:
22560627
15.

Tri- and tetrasubstituted pyrazole derivates: regioisomerism switches activity from p38MAP kinase to important cancer kinases.

Abu Thaher B, Arnsmann M, Totzke F, Ehlert JE, Kubbutat MH, Schächtele C, Zimmermann MO, Koch P, Boeckler FM, Laufer SA.

J Med Chem. 2012 Jan 26;55(2):961-5. doi: 10.1021/jm201391u. Epub 2012 Jan 17.

PMID:
22185282
16.

Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.

Beckers T, Sellmer A, Eichhorn E, Pongratz H, Schächtele C, Totzke F, Kelter G, Krumbach R, Fiebig HH, Böhmer FD, Mahboobi S.

Bioorg Med Chem. 2012 Jan 1;20(1):125-36. doi: 10.1016/j.bmc.2011.11.023. Epub 2011 Nov 20.

PMID:
22169601
17.

Dual IGF-1R/SRC inhibitors based on a N'-aroyl-2-(1H-indol-3-yl)-2-oxoacetohydrazide structure.

Schmidt S, Preu L, Lemcke T, Totzke F, Schächtele C, Kubbutat MH, Kunick C.

Eur J Med Chem. 2011 Jul;46(7):2759-69. doi: 10.1016/j.ejmech.2011.03.065. Epub 2011 Apr 6.

PMID:
21524503
18.

Identification of Inhibitors of the Tyrosine Kinase c-Met by Structure-Based Virtual Screening.

Lemcke T, Dreher J, Rarey M, Totzke F, Schächtele C, Kubbutat MH, Kunick C.

Mol Inform. 2011 Mar 14;30(2-3):145-50. doi: 10.1002/minf.201000138. Epub 2011 Mar 17. No abstract available.

PMID:
27466768
19.

Discovery of 4-benzylamino-substituted α-carbolines as a novel class of receptor tyrosine kinase inhibitors.

Krug M, Wichapong K, Erlenkamp G, Sippl W, Schächtele C, Totzke F, Hilgeroth A.

ChemMedChem. 2011 Jan 3;6(1):63-72. doi: 10.1002/cmdc.201000384.

PMID:
21140395
20.

Discovery and selectivity-profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors.

Krug M, Erlenkamp G, Sippl W, Schächtele C, Totzke F, Hilgeroth A.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6915-9. doi: 10.1016/j.bmcl.2010.10.004. Epub 2010 Oct 27.

PMID:
21035334

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