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Year Number of Results
2014 3
2015 3
2016 4
2017 3
2018 7
2019 2
2020 2
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23 results
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Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants.
Marek M, Shaik TB, Heimburg T, Chakrabarti A, Lancelot J, Ramos-Morales E, Da Veiga C, Kalinin D, Melesina J, Robaa D, Schmidtkunz K, Suzuki T, Holl R, Ennifar E, Pierce RJ, Jung M, Sippl W, Romier C. Marek M, et al. Among authors: melesina j. J Med Chem. 2018 Nov 21;61(22):10000-10016. doi: 10.1021/acs.jmedchem.8b01087. Epub 2018 Nov 8. J Med Chem. 2018. PMID: 30347148
Design of selective histone deacetylase inhibitors: rethinking classical pharmacophore.
Melesina J, Praetorius L, Simoben CV, Robaa D, Sippl W. Melesina J, et al. Future Med Chem. 2018 Jul 1;10(13):1537-1540. doi: 10.4155/fmc-2018-0125. Epub 2018 Jul 3. Future Med Chem. 2018. PMID: 29966452
Carbamates as Potential Prodrugs and a New Warhead for HDAC Inhibition.
King K, Hauser AT, Melesina J, Sippl W, Jung M. King K, et al. Among authors: melesina j. Molecules. 2018 Feb 2;23(2):321. doi: 10.3390/molecules23020321. Molecules. 2018. PMID: 29393896 Free PMC article.
Targeting histone deacetylase 8 as a therapeutic approach to cancer and neurodegenerative diseases.
Chakrabarti A, Melesina J, Kolbinger FR, Oehme I, Senger J, Witt O, Sippl W, Jung M. Chakrabarti A, et al. Among authors: melesina j. Future Med Chem. 2016 Sep;8(13):1609-34. doi: 10.4155/fmc-2016-0117. Epub 2016 Aug 30. Future Med Chem. 2016. PMID: 27572818 Free article. Review.
Synthesis and biochemical evaluation of two novel N-hydroxyalkylated cyclosporin A analogs.
Kahlert V, Prell E, Ohlenschläger O, Melesina J, Schumann M, Lücke C, Fischer G, Malešević M. Kahlert V, et al. Among authors: melesina j. Org Biomol Chem. 2018 Jun 13;16(23):4338-4349. doi: 10.1039/c8ob00980e. Org Biomol Chem. 2018. PMID: 29845172
Isoform-selective HDAC1/6/8 inhibitors with an imidazo-ketopiperazine cap containing stereochemical diversity.
Lecointre B, Narozny R, Borrello MT, Senger J, Chakrabarti A, Jung M, Marek M, Romier C, Melesina J, Sippl W, Bischoff L, Ganesan A. Lecointre B, et al. Among authors: melesina j. Philos Trans R Soc Lond B Biol Sci. 2018 Jun 5;373(1748):20170364. doi: 10.1098/rstb.2017.0364. Philos Trans R Soc Lond B Biol Sci. 2018. PMID: 29685969 Free PMC article.
Chiral Pool Synthesis, Biological Evaluation and Molecular Docking Studies of C-Furanosidic LpxC Inhibitors.
Dreger A, Kharwb O, Agoglitta O, Bülbül EF, Melesina J, Sippl W, Holl R. Dreger A, et al. Among authors: melesina j. ChemMedChem. 2019 Apr 17;14(8):871-886. doi: 10.1002/cmdc.201900068. Epub 2019 Mar 12. ChemMedChem. 2019. PMID: 30801965
Proline-based hydroxamates targeting the zinc-dependent deacetylase LpxC: Synthesis, antibacterial properties, and docking studies.
Kalinin DV, Agoglitta O, Van de Vyver H, Melesina J, Wagner S, Riemann B, Schäfers M, Sippl W, Löffler B, Holl R. Kalinin DV, et al. Among authors: melesina j. Bioorg Med Chem. 2019 May 15;27(10):1997-2018. doi: 10.1016/j.bmc.2019.03.056. Epub 2019 Mar 30. Bioorg Med Chem. 2019. PMID: 30954331
Synthesis, Crystallization Studies, and in vitro Characterization of Cinnamic Acid Derivatives as SmHDAC8 Inhibitors for the Treatment of Schistosomiasis.
Bayer T, Chakrabarti A, Lancelot J, Shaik TB, Hausmann K, Melesina J, Schmidtkunz K, Marek M, Erdmann F, Schmidt M, Robaa D, Romier C, Pierce RJ, Jung M, Sippl W. Bayer T, et al. Among authors: melesina j. ChemMedChem. 2018 Aug 10;13(15):1517-1529. doi: 10.1002/cmdc.201800238. Epub 2018 Jul 4. ChemMedChem. 2018. PMID: 29806110
A Novel Class of Schistosoma mansoni Histone Deacetylase 8 (HDAC8) Inhibitors Identified by Structure-Based Virtual Screening and In Vitro Testing.
Simoben CV, Robaa D, Chakrabarti A, Schmidtkunz K, Marek M, Lancelot J, Kannan S, Melesina J, Shaik TB, Pierce RJ, Romier C, Jung M, Sippl W. Simoben CV, et al. Among authors: melesina j. Molecules. 2018 Mar 2;23(3):566. doi: 10.3390/molecules23030566. Molecules. 2018. PMID: 29498707 Free PMC article.
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