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Structure-based design, synthesis and in vitro characterization of potent 17beta-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone.
Möller G, Deluca D, Gege C, Rosinus A, Kowalik D, Peters O, Droescher P, Elger W, Adamski J, Hillisch A. Möller G, et al. Among authors: hillisch a. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6740-4. doi: 10.1016/j.bmcl.2009.09.113. Epub 2009 Oct 3. Bioorg Med Chem Lett. 2009. PMID: 19836949
The lab oddity prevails: discovery of pan-CDK inhibitor (R)-S-cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY 1000394) for the treatment of cancer.
Lücking U, Jautelat R, Krüger M, Brumby T, Lienau P, Schäfer M, Briem H, Schulze J, Hillisch A, Reichel A, Wengner AM, Siemeister G. Lücking U, et al. Among authors: hillisch a. ChemMedChem. 2013 Jul;8(7):1067-85. doi: 10.1002/cmdc.201300096. Epub 2013 May 13. ChemMedChem. 2013. PMID: 23671017
Structure-Permeability Relationship of Semipeptidic Macrocycles-Understanding and Optimizing Passive Permeability and Efflux Ratio.
Le Roux A, Blaise É, Boudreault PL, Comeau C, Doucet A, Giarrusso M, Collin MP, Neubauer T, Kölling F, Göller AH, Seep L, Tshitenge DT, Wittwer M, Kullmann M, Hillisch A, Mittendorf J, Marsault E. Le Roux A, et al. Among authors: hillisch a. J Med Chem. 2020 Jul 9;63(13):6774-6783. doi: 10.1021/acs.jmedchem.0c00013. Epub 2020 May 26. J Med Chem. 2020. PMID: 32453569
Target 2035 - update on the quest for a probe for every protein.
Müller S, Ackloo S, Al Chawaf A, Al-Lazikani B, Antolin A, Baell JB, Beck H, Beedie S, Betz UAK, Bezerra GA, Brennan PE, Brown D, Brown PJ, Bullock AN, Carter AJ, Chaikuad A, Chaineau M, Ciulli A, Collins I, Dreher J, Drewry D, Edfeldt K, Edwards AM, Egner U, Frye SV, Fuchs SM, Hall MD, Hartung IV, Hillisch A, Hitchcock SH, Homan E, Kannan N, Kiefer JR, Knapp S, Kostic M, Kubicek S, Leach AR, Lindemann S, Marsden BD, Matsui H, Meier JL, Merk D, Michel M, Morgan MR, Mueller-Fahrnow A, Owen DR, Perry BG, Rosenberg SH, Saikatendu KS, Schapira M, Scholten C, Sharma S, Simeonov A, Sundström M, Superti-Furga G, Todd MH, Tredup C, Vedadi M, von Delft F, Willson TM, Winter GE, Workman P, Arrowsmith CH. Müller S, et al. Among authors: hillisch a. RSC Med Chem. 2021 Dec 3;13(1):13-21. doi: 10.1039/d1md00228g. eCollection 2022 Jan 27. RSC Med Chem. 2021. PMID: 35211674 Free PMC article.
Design and Preclinical Characterization Program toward Asundexian (BAY 2433334), an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic Disorders.
Roehrig S, Ackerstaff J, Jiménez Núñez E, Teller H, Ellerbrock P, Meier K, Heitmeier S, Tersteegen A, Stampfuss J, Lang D, Schlemmer KH, Schaefer M, Gericke KM, Kinzel T, Meibom D, Schmidt M, Gerdes C, Follmann M, Hillisch A. Roehrig S, et al. Among authors: hillisch a. J Med Chem. 2023 Sep 14;66(17):12203-12224. doi: 10.1021/acs.jmedchem.3c00795. Epub 2023 Sep 5. J Med Chem. 2023. PMID: 37669040 Free PMC article.
54 results