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Publikationen

115. 1-deoxy-D-xylulose 5-phosphate reductoisomerase (DXR) as target for anti Toxoplasma gondii agents: crystal structure, biochemical characterisation and biological evaluation of inhibitors. Mazzone, F.; Hoeppner, A.; Reiners, J.; Gertzen, C. G.; Applegate, V.; Abdullaziz, M. A.; Gottstein, J.; Degrandi, D.; Wesemann, M.; Kurz, T.; Smits, S.; Pfeffer, K. Biochemical Journal 2024, Doi: 10.1042/BCJ20240110.

114. Novel Histone Deacetylase (HDAC) Inhibitor Induces Apoptosis and Suppresses Invasion via E-Cadherin Upregulation in Pancreatic Ductal Adenocarcinoma (PDAC). Schiedlauske, K.; Deipenbrock, A.; Pflieger, M.; Hamacher, A.; Hänsel, J.; Kassack, M.U.; Kurz, T.; Teusch, N.E. Pharmaceuticals 2024, 17, 752. Doi: 10.3390/ph17060752

113. Synthesis and biological evaluation of hydantoin derivatives as potent antiplasmodial agents. Chin, E.Z.; Chang, W.J.; Tan, H.Y., Liew, S.Y.; Lau, Y.L.; Ng, Y.L.; Nafiah, M.A.; Kurz, T.; Tan, S.T. Bioorg. Med. Chem. Lett. 2024, 103, 129701. Doi: 10.1016/j.bmcl.2024.129701

112. Differential effects of HDAC6 inhibition versus knockout during hepatic ischemia-reperfusion injury highlight importance of HDAC6 C-terminal zinc-finger ubiquitin-binding domain. Concors, S.J.; Hernandez, P.T.; O’Brien, C.; DePaolo, J.; Murken, D.R.; Aufhauser, D.D.; Wang, Z.; Xiong, Y.; Krumeich, L.; Ge, G.; Beier, U.H.; Bhatti, T.R.; Kozikowski, A.P.; Avelar, L.; Kurz, T.; Hancock, W.W.; Levine, M.H. Transplantation 2024.

111. Activity of alkoxyamide-based histone deacetylase inhibitors against Plasmodium falciparum malaria parasites. Dawood, W.A.; Fisher, G.M.; Kinnen, F.J.M.; Anzenhofer, C.; Skinner-Adams, T.; Avelar, L.A.; Asfaha, Y.; Kurz, T.; Andrews, K.T. Experimental Parasitology 2024, 258, 108716. Doi: 10.1016/j.exppara.2024.108716

110. Reverse N‑Substituted Hydroxamic Acid Derivatives of Fosmidomycin Target a Previously Unknown Subpocket of 1‑Deoxy-D-xylulose 5‑Phosphate Reductoisomerase (DXR). Abdullaziz, M.A.; Takada, S.; Illarionov, B.; Pessanha de Carvalho, L.; Sakamoto, Y.; Hofmann, S.; Knak, T.; Kiffe-Delf, A.L.; Mazzone, F.; Pfeffer, K.; Kalscheuer, R.; Bacher, A.; Held, J.; Fischer, F.; Tanaka, N.; Kurz, T. ACS Infect. Dis. 2024. Doi: 10.1021/acsinfecdis.4c00100

109. 5-(Trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based highly selective class IIa HDAC inhibitors exhibit synergistic anticancer activity in combination with bortezomib. Asfaha, Y.; Bollmann, L.M.; Skerhut, A.J.; Fischer, F.; Horstick, N.; Roth, D.; Wecker, M.; Mammen, Ch.; Smits, S.H.J.; Fluegen, G.; Kassack, M.U.; Kurz, T. Eur. J. Med. Chem. 2024, 263, 115907. Doi.org/10.1016/j.ejmech.2023.115907.

108. Regulation of STING activity in DNA sensing by ISG15 modification. Lin, C.; Kuffour, E. O; Fuchs, N. V.; Gertzen, C. G. W.; Kaiser, J.; Hirschenberger, M.; Tang, X.; Xu, H. C.; Michel, O.; Tao, R.; Haase, A.; Martin, U.; Kurz, T.; Drexler, I.; Görg, B.; Lang, P. A.; Luedde, T.; Sparrer, K. M. J.; Gohlke, H.; König, R.; Münk, C. Cell Rep2023, 20; 42(11):113277. Doi: 10.1016/j.celrep.2023.113277

107. Quantification of Plasmodium falciparum HPR-2 as an alternative method to [3H] hypoxanthine incorporation to measure the parasite reduction ratio in vitro. de Carvalho, L.P.; Niepoth, E.; Mavraj-Husejni, A.; Kreidenweiss, A.; Herrmann, J.; Müller, R.; Knaab, T.; Burckhardt, B.B.; Kurz, T.; Held, J. Int J Antimicrob Agents2023, 62 (3), 106894. Doi: 10.1016/j.ijantimicag.2023.106894.

106. Over 40 Years of Fosmidomycin Drug Research: A Comprehensive Review and Future Opportunities. Knak, T.; Abdullaziz, M.A.; Höfmann, S.; Alves Avelar, L.A.; Klein, S.; Martin, M.; Fischer, M.; Tanaka, N. and Kurz, T. Pharmaceuticals 2022, 15, 1553. https://doi.org/10.3390/ph15121553

105. The Novel Class IIa Selective Histone Deacetylase Inhibitor YAK540 Is Synergistic with Bortezomib in Leukemia Cell Lines. Bollmann, L.M.; Skerhut, A.J.; Asfaha, Y.; Horstick, N.; Hanenberg, H.; Hamacher, A.; Kurz, T.; and Kassack, M.U. Int. J. Mol. Sci. 202223(21), 13398. Doi.org/10.3390/ijms232113398

104. Establishment and evaluation of a dual HDAC / BET inhibitor as a therapeutic option for germ cell tumors and other urological malignancies. Burmeister, A.; Stephan, A.;   Avelar, LAA.; Müller, M.R.;  Seiwert, A.; Höfmann, S.; Fischer, F.; Torres-Gomez , H.;  Hoffmann, M.J.;  Niegisch , G.; Bremmer , F.; Petzsch, P.; Köhrer, K.; Albers, P.; Kurz, T.;  Skowron, M.A. and  Nettersheim, D. Mol Cancer Ther2022, 21(11),1674-1688. DOI: 10.1158/1535-7163.MCT-22-0207.

103. Total Synthesis of the Antimycobacterial Natural Product Chlorflavonin and Analogs via a Late-Stage Ruthenium(II)-Catalyzed ortho-C(sp2)-H-Hydroxylation. Berger, A.; Knak, T.; Kiffe-Delf, A.; Mudrovcic, K.; Singh, V.; Njoroge, M.; Burckhardt, B.B.; Gopalswamy, M.; Lungerich, B.; Ackermann, L.; Gohlke, H.; Chibale, K.; Kalscheuer, R. and Kurz, T. Pharmaceuticals. 2022,15(8), 984-989. doi.org: 10.3390/ph15080984

102. Development of a First-in-Class Small-Molecule Inhibitor of the C-Terminal Hsp90 Dimerization. Bhatia, S., Spanier, L., Bickel, D., Dienstbier, N., Woloschin, V., Vogt, M., Pols, H., Lungerich, B., Reiners, J., Aghaallaei, N., Diedrich, D., Frieg, B., Diecks, J.S., Bopp, B., Lang, F., Gopalswamy, M., Loschwitz, J., Bajohgli, B., Skokowa, J., Borkhardt, A., Hauer, J., Hansen, F.K., Smits, S.H.J.,  Jose, J., Gohlke, H., and Kurz, T. ACS Cent. Sci. 2022, 8(5), 636–655. doi.org/10.1021/acscentsci.2c00013

101. Assessing the Anthelmintic Candidates BLK127 and HBK4 for Their Efficacy on Haemonchus contortus Adults and Eggs, and Their Hepatotoxicity and Biotransformation. Zajíčková, M., Prchal, L., Vokřál, I., Nguyen, L.T., Kurz, T., Gasser. R., Bednářová, K., Mičundová, M., Lungerich, B., Michel, O., and Skálová, L. Pharmaceutics. 202214(4), 754. doi.org/10.3390/pharmaceutics14040754

100. QSAR Classification Models for Prediction of Hydroxamate Histone Deacetylase Inhibitor Activity against Malaria Parasites. Hesping, E., Chua, M.J., Pflieger, M., Qian, Y., Dong, L., Bachu, P., Liu, L., Kurz, T., Fisher, G.M., Skinner-Adams, T.S., Reid, R.C., Fairlie, D.P., Andrews, K.T., and Gorse, A.J.P. ACS Infect. Dis. 2022, 8(1), 106–117. doi:org/10.1021/acsinfecdis.1c00355

99. Antiproliferation and Antiencystation Effect of Class II Histone Deacetylase Inhibitors on Acanthamoeba castellanii. Chu, Ki-Back; Lee, Hae-Ahm; Pflieger, Marc; Fischer, Fabian; Asfaha, Yodita; Alves Avelar, Leandro A.; Skerhut, Alexander; Kassack, Matthias U.; Hansen, Finn K.; Schöler, Andrea; Kurz, Thomas; Kim, Min-Jeong; Moon, Eun-Kyung; Quan, Fu-Shi. ACS Infect. Dis. 2022, Doi.org/10.1021/acsinfecdis.1c00390

98. Designing HDAC-PROTACs: lessons learned so far. Fischer, F., Alves Avelar, L.A., Murray, L., and Kurz, T. Future Medicinal Chemistry. 2021 0 0:0. Doi.org/10.4155/fmc-2021-0206

97. Three Small Molecule Entities (MPK18, MPK334 and YAK308) with Activity against Haemonchus contortus In Vitro. Taki, A.C., Abdul Jabbar, Kurz, T., Lungerich, B., Ma, G., Byrne, J.J., Pflieger, M, Asfaha, Y., Fischer, F., Chang, B.C.H., Sleebs, B.E., and Gasser, R.B. Molecules. 202126(9), 2819. Doi.org/10.3390/molecules26092819

96. 3-Hydroxy-propanamidines, a New Class of Orally Active Antimalarials Targeting Plasmodium falciparum. Knaab, T.C., Held, J., Burckhardt, B.B.,  Rubiano, K., Okombo, J., Yeo, T., Mok, S., Uhlemann, A., Lungerich, B., Fischli, C., Carvalho, L.P., Mordmüller, B., Wittlin, S., Fidock, D.A., Kurz, T. Journal of Medicinal Chemistry Article ASAP. 2021. DOI: 10.1021/acs.jmedchem.0c01744.

95. Synergistic induction of apoptosis in resistant head and neck carcinoma and leukemia by alkoxyamide-based histone deacetylase inhibitors. Avelar, L.A.A., Schrenk, C., Sönnichsen, M., Hamacher, A., Hansen, F.K., Schliehe-Diecks, J., Borkhardt, A., Bhatia, S., Kassack, M.U. and Kurz, T. Eur. J. Med. Chem. 2021, 211, 113095. DOI: 10.1016/j.ejmech.2020.113095

94. Oxa analogues of nexturastat A demonstrate improved HDAC6 selectivity and superior antileukaemia activity. Pflieger, M., Sönnichsen, M., Horstick-Muche, N., Yang, J., Schliehe-Diecks, J., Schöler, A., Borkhardt, A., Hamacher, A., Kassack, M.U., Hansen, F.K., Bhatia, S., Kurz. T. ChemMedChem. 2021, 16, 1-7. Doi.org/10.1002/cmdc.202001011

93. Synthesis of thiazolyl-based hydroxamic acids as histone deacetylase inhibitors (JB-11279KP).
Asfaha, Y., Skerhut, A. J., Alves Avelar, L. A., Horstick-Muche, N., Lungerich, B., Klinken, S., Kassack, M. U., Kurz, T. Arkivoc 2020,  228 – 241. doi:org/10.24820/ark.5550190.p011.279

92. An ELISA method to assess HDAC inhibitor-induced alterations to P. falciparum histone lysine acetylation. Hespinga, E., Skinner-Adamsa T. S., Fishera, G. M.,Kurz, T., Andrewsa, K. T. International Journal for Parasitology: Drugs and Drug Resistance. 2020, (14), 249-256. doi: 10.1016/j.ijpddr.2020.10.010

91. Priming with HDAC Inhibitors Sensitizes Ovarian Cancer Cells to Treatment with Cisplatin and HSP90 Inhibitors. Moita, A. J. R., Bandolik, J. J.,  Hansen F. K.  , Kurz. T., Hamacher A., Kassack, M. U. Int. J. Mol. Sci. 2020, 21(21), 8300-8322; doi:org/10.3390/ijms21218300

90. Application of histone deacetylase inhibitors MPK472 and KSK64 as a potential treatment option for Acanthamoeba keratitis. Lee, H., Park, S., Chu, K., Quan, F., Kurz, T., Pflieger, M., Moon, E. Antimicrobial Agents and Chemotherapy. 202064(12), e01506-20. doi: 10.1128/AAC.01506-20

89. Cell type-dependent escape of capsid inhibitors by simian immunodeficiency virus SIVcpz. Twizerimana, A. P., Scheck, R., Becker, D., Zhang, Z., Wammers, V., Avelar, L., Pflieger, M., Häussinger, D., Kurz, T., Gohlke, H. and Münk C. Journal of Virology. 2020, 94 (23), e01338- e01358; doi:10.1128/JVI.01338-20

88. In Vitro Assessment of the Genotoxic Hazard of Novel Hydroxamic Acid- and Benzamide-Type Histone Deacetylase Inhibitors (HDACi). Friedrich, A.,  Assmann, A., Schumacher, L.,  Stuijvenberg, J.v., U., K., Matthias, Schulz,  W., A.,  Roos, W., P., Hansen, F, K.,  Pflieger, M., Kurz, T. and Fritz, G.  Int. J. Mol. Sci. 2020, 21, 4747; doi.org/10.3390/ijms21134747

87. ARID1A Regulates Transcription and the Epigenetic Landscape via POLE and DMAP1 While ARID1A Deficiency or Pharmacological Inhibition Sensitizes Germ Cell Tumor Cells to ATR Inhibition Kurz,L. , Miklyaeva, A., Skowron M. A., Overbeck, N., Poschmann, G., Becker, T., Eul, K., Kurz, T., Schönberger, S., Calaminus, G., Stühler, K., Dykhuizen, E., Albers, P. and Nettersheim, D. Cancers 2020, 12, 905; doi:10.3390/cancers12040905

86. Inhibition of the Yersinia pestis Methylerythritol Phosphate Pathway of Isoprenoid Biosynthesis by α-Phenyl-Substituted Reverse Fosmidomycin Analogues. Ball, H. S., Girma, M., Zainab, M., Riley, H., Behrendt, C. T., Lienau, C., Konzuch, S., Alves Avelar, L. A., Lungerich, B., Soojhawon, I., Noble, S. M., Kurz,  T. and Couch, R. D. ACS Omega. 2020, 5, 5170-5175. doi: 10.1021/acsomega.9b04171.

85. Novel alkoxyamide-based histone deacetylase inhibitors reverse cisplatin resistance in             chemoresistant cancer cells. Asfaha, Y., Schrenk, C., Alves Avelar, L. A., Lange, F., Wang, C., BandoliK, J. J., Alexandra, H., Kassack, M. U., Kurz, T. Bioorganic & Medicinal Chemistry. 2020, 28 (1), 115108. Doi: 10.1016/j.bmc.2019.115108.

84. Synthesis of Peptoid-Based Class I-Selective Histone Deacetylase Inhibitors with Chemosensitizing Properties. Krieger, V., Hamacher, A., Cao, F., Stenzel, K., Gertzen, C. G. W., Scha, L., Bner, K., Kurz, T., Gohlke, H., Dekker, F. J.,  Kassack, M. U., and Hansen, F. K. J. Med. Chem. 2019, 24, 11260–11279. Doi:10.1021/acs.jmedchem.9b01489

83. Recent advances in class IIa histone deacetylases research. Asfaha, Y., Schrenk, C., Alves Avelar, L. A., Hamacher, A., Pflieger, M., Kassack, M. U., Kurz, T. Bioorg. Med. Chem. 2019, 27, 115087. Doi: 10.1016/j.bmc.2019.115087.

82. Novel α, β-unsaturated hydroxamic acid derivatives overcome cisplatin resistance. Pflieger, M ., Hamacher, A. , Öz, T. , Horstick-Muche, N., Boesen, B., Schrenk, C. , Kassack, M. U. , Kurz, T.      Bioorganic & Medicinal Chemistry. 2019, 27, 115036. Doi: 10.1016/j.bmc.2019.07.052

81. Structure-Based Design of Selective Histone Deacetylase 6 Zinc Binding Groups. Alves Avelar, L. A., Ruzic, D., Djokovic, N., Kurz, T., Nikolic, K. J. Biomol. Struct. Dyn. 2019, 14, 1-12. Doi: 10.1080/07391102.2019.1652687.

80. Novel reverse thia-analogs of fosmidomycin: Synthesis and antiplasmodial activity. Lienau, C., Gräwert, T., Alves Avelar, L. A., Illarionov, B., Held, J., Knaab, T. C., Lungerich, B., van Geelen, L., Meier, D., Geissler, S., Cynis, H., Riederer, U., Buchholz, M., Kalscheuer, R., Bacher, A., Mordmüller, B., Fischer, M., Kurz, T. Eur. J. Med. Chem. 2019, 181, 111555. doi: Doi: 10.1016/j.ejmech.2019.07.058.

79. Phenotypic screening of the ‘Kurz-box’ of chemicals identifies two compounds (BLK127 and HBK4) with anthelmintic activity in vitro against parasitic larval stages of Haemonchus contortus. Nguyen, L. T., Kurz, T., Preston, S., Brueckmann, H., Lungerich, B., Herath, H. M. P. D., Koehler, A. V., Wang, T., Skálová, L., Jabbar, A., Gasser, R. B. Parasit Vectors. 2019, 12, 191-199. Doi: 10.1186/s13071-019-3426-7.

78. Histone deacetylase inhibitor LMK235 attenuates vascular constriction and aortic remodelling in    hypertension. Choi, S. Y., Kee, H. J., Sun, S., Seok, Y. M., Ryu, Y., Kim, G. R., Kee, S. J., Pflieger, M., Kurz, T., Kassack, M. U., Jeong, M. H. J. Cell Mol. Med. 2019, 23, 2801-2812. Doi: 10.1111/jcmm.14188.

77. Class I histone deacetylase inhibitor MS-275 attenuates vasoconstriction and inflammation in angiotensin II-induced hypertension. Ryu, Y., Kee, H. J., Sun, S., Seok, Y. M., Choi, S. Y., Kim, G. R., Kee, S. J., Pflieger, M., Kurz, T., Kim, H. S., Jeong, M. H. PloS one. 2019, 14, e0213186. Doi: 10.1371/journal.pone.0213186

76. Structure-Activity and Structure-Toxicity Relationships of Novel Peptoid‐Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity. Mackwitz, M. K. W., Hesping, E., Antonova-Koch, Y., Diedrich, D., Woldearegai, T. G., Skinner-Adams, T., Clarke, M., Schöler, A., Limbach, L., Kurz, T., Winzeler, E. A., Held, J., Andrews, K. T., Hansen, F. K. ChemMedChem. 2019, 14, 1-16. DOI: 10.1002/cmdc.201800808

75. Histone deacetylase inhibitor LMK235 attenuates vascular constriction and aortic remodelling in    hypertension. Choi, S. Y., Kee, H. J., Sun, S., Seok, Y. M., Ryu, Y., Kim, G. R., Kee, S. J., Pflieger, M., Kurz, T., Kassack, M. U., Jeong, M. H. J. Cell. Mol. Med. 2019, 23, 2801-2812. DOI: 10.1111/jcmm.14188.

74. 8-Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual-Stage Antiplasmodial Activity. Leven, M., Held, J., Duffy, S., Alves Avelar, L. A., Meister, S., Delves, M., Plouffe, D.,   Kuna, K., Tschan, S., Avery, V. M., Winzeler, E. A., Mordmüller, B., Kurz, T. ChemMedChem. 2019, 14, 501-511. DOI: 10.1002/cmdc.201800691

73. Discovery of the first-in-class dual histone deacetylase-proteasome inhibitor. Bhatia, S., Krieger, V., Groll, M., Osko, J. D., Reßing, N., Ahlert, H., Borkhardt, A., Kurz, T., Christianson, D. W., Hauer, J.,  Hansen, F .K. J. Med. Chem. 2018, 61, 10299-20309. DOI: 10.1021/acs.jmedchem.8b01487.

72. Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity. Reßing, N., Marquardt, V., Gertzen, C. G. W,, Schöler, A., Schramm, A., Kurz, T., Gohlke, H., Aigner, A., Remke, M., Hansen, F. K. Medchemcomm. 2018, 10, 1109-1115. Doi: 10.1039/c8md00454d.

71. One-pot, multi-component synthesis and structure-activity relationships of peptoid-based his­tone deacetylase (HDAC) inhibitors targeting malaria parasites. Diedrich, D., Stenzel, K., Hesping, E.,         Antonova-Koch, Y., Gebru, T., Duffy, S., Fisher, G., Schöler, A., Meister, S., Kurz, T., Avery V. M., Winzeler, E. A., Held, J., Andrews, K. T. Hansen, F. K. Eur. J. Med. Chem. 2018, 158, 801-813. Doi: 10.1016/j.ejmech.2018.09.018.

70. HDAC6-Selective Phenylhydroxamate Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity. Porter, N. J., Osko, J. D., Diedrich, D., Kurz, T., Hooker, J. M., Hansen, F. K., Christianson, D. W. J. Med. Chem. 2018, 61, 8054-8060. Doi: 10.1021/acs.jmedchem.8b01013.

69. Effects of novel HDAC inhibitors on urothelial carcinoma cells. Kaletsch, A., Pinkerneil, M., Hoffmann, M. J., Jaguva Vasudevan, A. A., Wang, C., Hansen, F. K., Wiek, C., Hanenberg, H., Gertzen, C., Gohlke, H., Kassack, M. U., Kurz, T., Schulz, W., Niegisch, G. Clin. Epigenetics. 2018, 10, 100-118. Doi: 10.1186/s13148-018-0531-y.

68. Targeting HSP90 dimerization via the C-terminus is effective in imatinib resistant CML and lacks the heat shock Response. Bhatia, S., Diedrich, D., Frieg, F., Ahlert, H., Stein, S., Bopp, B., Lang, F., Zang, T., Kroeger, T., Ernst, T., Koegler, G., Krieg, A., Luedeke, S., Kunkel, H., Rodrigues Moita, A. J., Kassack, M. U., Marquardt, V., Opitz, F., Oldenburg, M., Remke, M., Babor, F., Grez, M., Hochhaus, A., Borkhardt, A., Groth, G., Nagel-Steger, L., Jose, J., Kurz, T., Gohlke, H., Hansen, F. K., Hauer, J. Blood. 2018, 132, 307-320 DOI: 10.1182/blood-2017-10-810986.

67. Design and Synthesis of Terephthalic Acid-Based Histone Deacetylase Inhibitors with Dual-Stage Anti-Plasmodium Activity. Stenzel, K., Chua, M. J., Duffy, S., Antonova-Koch, Y., Meister, S., Hamacher, A., Kassack, M. U., Winzeler, E., Avery, V. M., Kurz, T., Andrews, K. T., Hansen, F. K. Chem. Med. Chem. 2017, 12, 1627-1636. Doi: 10.1002/cmdc.201700360.

66. 3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally. Leven, M., Knaab, T., Held, J. K., Duffy, S., Meister, S., Fischli, C., Meitzner, D., Lehmann, U., Lungerich, B., Kuna, K., Stahlke, P., Delves, M. J.,      Buchholz, M., Winzeler E. A., Avery, V. M., Mordmüller, B., Wittlin, S., Kurz, T. J. Med. Chem. 2017, 60, 5036-5044. Doi: 10.1021/acs.jmedchem.7b00140.

65. Alkoxyurea-based Histone Deacetylase Inhibitors Increase Cisplatin Chemosensitivity.
Stenzel, K., Hamacher, A., Hansen, F. K., Gertzen, C. G. W., Senger, J., Marquardt, V., Marek, .L, Marek, M., Romier, C., Remke, M., Jung, M., Gohlke, H., Kassack, M. U., Kurz, T. J. Med. Chem. 2017, 60, 5334-5348. DOI: 10.1021/acs.jmedchem.6b01538.

64. Design, multicomponent synthesis and anticancer activity of a focused library of HDAC inhibitors with peptoid-based cap groups. Krieger, V., Hamacher, A., Gertzen, C. G. W., Senger, J., Zwinderman, M. R. H., Marek, M., Romier, C., Dekker, F. J., Kurz, T., Jung, M., Gohlke, H.,
Kassack, M. U., Hansen, F. K. J. Med. Chem. 2017, 60, 5493-5506. DOI: 10.1021/acs.jmedchem.7b00197.

63. Isophthalic acid-based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni. Stenzel, K., Chakrabarti, A., Melesina, J., Hansen, F. K., Lancelot, J., Herkenhöhner, S., Lungerich, B., Marek, M., Romier, C., Pierce, R. J., Sippl, W., Jung, M.; Kurz, T. Arch. Pharm. 2017, 350, e170000ß96. DOI: 10.1002/ardp.201700096.

62. Design and Synthesis of Novel Anti-Plasmodial Histone Deacetylase Inhibitors Containing an Alkoxyamide Connecting Unit. Alves Avelar, L. A., Held, J., Engel, J. A., Sureechatchaiyan. P., Hansen, F. K., Hamacher, A., Kassack, M. U., Mordmüller, B., Andrews, K. T., Kurz, T. Archiv Pharmazie. 2017, 305, e1600347. DOI: 10.1002/ardp.201600347.

61. α-Aminoxy Peptoids: A Unique Peptoid Backbone with a Preference for Cis-Amide Bonds. Krieger, V., Ciglia, E., Thoma, R., Vasylyeva, V., Frieg, B., de Sousa Amadeu, N., Kurz, T., Janiak, C., Gohlke, H., Hansen, F. K. Chemistry. 2017, 23, 3699-3707. DOI: 10.1002/chem.201605100.

60. HDAC4: a key factor underlying brain developmental alterations in CDKL5 disorder. Trazzi, S., Fuchs, C., Viggiano, R., De Franceschi, M., Valli, E., Jedynak, P., Hansen, F. K., Perini, G., Rimondini, R., Kurz, T., Bartesaghi, R., Ciani, E. Hum. Mol. Genet. 2016, 25, 3887-3907. DOI: 10.1093/hmg/ddw231.

59. α-Aminoxy oligopeptides: synthesis, secondary structure and cytotoxicity of a novel class of anti­cancer foldamers. Diedrich, D., Moita, A. J., Rüther, A., Frieg, B., Reiss, G. J., Hoeppner, A., Kurz, T., Gohlke, H., Lüdeke, S., Kassack, M. U., Hansen, F. K. Chemistry. 2016, 22, 17600-17611. Doi: 10.1002/chem.201602521.

58. Class I HDACs Specifically Regulate E-cadherin Expression in Human Renal Epithelial Cells. Choi, S. Y., Kee, H. J., Kurz, T., Hansen, F. K., Ryu, Y., Kim, G. R., Lin, M. Q., Jin, L., Piao, Z. H., Jeong, M. H. J. Cell Mol. Med. 2016, 20, 2289-2298. DOI: 10.1111/jcmm.12919.

57. Rational design and diversity-oriented synthesis of peptoid-based selective HDAC6 inhibitors. Diedrich, D., Hamacher, A., Gertzen, C. G., Alves Avelar, L. A., Reiss, G. J., Kurz, T., Gohlke, H., Kassack, M. U., Hansen, F. K. Chem. Commun. 2016, 52, 3219-3222. Doi: 10.1039/c5cc10301k.

56. HDAC5 controls the functions of Foxp3+ T-regulatory and CD8+ T cells. Xiao, H., Jiao, J., Wang, L., O’Brien, S., Newick, K., Wang, L. C., Falkensammer, E., Liu, Y., Han, R., Kapoor, V., Hansen, F. K., Kurz, T., Hancock, W. W., Beier, U. H. Int. J. Cancer. 2016, 138, 2477-2486. Doi: 10.1002/ijc.29979.

55. Inhibition of the Non-Mevalonate Isoprenoid Pathway by Reverse Hydrox­amate Analogues of      Fosmidomycin. Lienaua, C., Konzucha, S., Gräwertb, T., Illarionovb, B., Bacherc, Adelbert.,  Fischerb, M., Tanakad, N., Kurz,T. Procedia Chemistry. 2015, 14, 108-116. Doi.org/10.1016/j.proche.2015.03.016

54. Histone deacetylase inhibition attenuates cardiac hypertrophy and fibrosis through acetylation of
 mineralocorticoid receptor in spontaneously hypertensive rats. Kang, S. H., Seok, Y. M., Song, M. j., Lee, H. A., Kurz, T., Kim, I. Mol. Pharm. 2015, 87, 782-791. DOI: 10.1124/mol.114.096974.

53. Prodrugs of Reverse Fosmidomycin Analogues. Brücher, K., Gräwert, T., Konzuch, S., Held, J., Lienau, C., Behrendt, C., Illarionov, B., Maes, L., Bacher, A., Wittlin, S., Mordmüller, B., Fischer, M., Kurz, T. J. Med. Chem. 2015, 58, 2025-2035. DOI: 10.1021/jm5019719.

52. Binding modes of reverse fosmidomycin analogs towards the antimalarial target IspC. Konzuch, S., Umeda, T., Held, J., Hähn, S., Brücher, K., Lienau, C., Behrendt, C., Gräwert, T., Bacher, A., Illarionov, B., Fischer, M., Mordmüller, B., Tanaka, N., Kurz, T.  J. Med. Chem. 2014, 57, 8827-8838. DOI: 10.1021/jm500850y.

51. Blood Schizontocidal and Gametocytocidal Activity of 3-Hydroxy-N′ arylidenepropanehydrazonamides: A New Class of Antiplasmodial Compounds. Leven, M., Held, J., Duffy, S., Tschan, S., Sax, S., Kamber, J., Frank, W., Kuna, K., Geffken, D., Siethoff, C., Barth, S., Avery, V. M., Wittlin, S., Mordmüller, B., Kurz, T. J. Med. Chem. 2014, 57, 7971-7976. DOI: 10.1021/jm500811p.

50. Discovery of HDAC Inhibitors with Potent Activity Against Multiple Malaria Parasite Life Cycle Stages. Hansen, F. K., Sumanadasa, S. D., Stenzel, K., Duffy, S., Meister, S., Marek, L., Schmetter, R., Kuna, K., Hamacher, A., Mordmüller, B., Kassack, M. U., Winzeler, E. A., Avery, V. M., Andrews, K. T., Kurz, T. Eur. J. Med. Chem. 2014, 23, 204-213. Doi: 10.1016/j.ejmech.2014.05.050.

49. Lysine acetylation in sexual stage malaria para­sites is a target for antimalarial small molecules.   Trenholme, K., Marek, L., Duffy, S., Pradel, G., Fisher, G., Hansen, F. K., Skinner-Adams, T. S.,          Butterworth, A., Ngwa, C. J., Moecking, J., Goodman, C. D., McFadden, G. I., Sumanadasa, S. D., Fairlie, D. P., Avery, V. M., Kurz, T., Andrews, K. T. Antimicrob. Agents Chemother. 2014, 58, 3666-3678. Doi: 10.1128/AAC.02721-13.

48. Design, Synthesisand Conformational Analysis of Trispyrimidonamides as α-Helix Mimetics. Spanier, L., Ciglia, E., Hansen, F. K., Kuna, K., Frank, W., Gohlke, H., Kurz, T. J. Org. Chem. 2014, 79, 1582-1593. DOI: 10.1021/jo402353z.

47. Synthesis, antimalarial properties and SAR studies of alkoxyurea-based HDAC inhibitors. Hansen, F. K., Skinner-Adams, T. S., Duffy, S., Marek, L., Sumanadasa, S. D. M., Kuna, K., Held, J., Avery, V. M., Andrews, K. T., Kurz, T. Chem. Med. Chem. 2014, 9, 665-670. DOI: 10.1002/cmdc.201300469.

 

46. IspC as Target for Antiinfective Drug Discovery: Synthesis, Enantiomeric Separation, and Structural Biology of Fosmidomycin Thia Isosters.
Kunfermann, A., Lienau, C., Illarionov, B., Held, J., Gräwert, T., Behrendt, C. T., Werner, P., Hähn, S., Eisenreich, W., Riederer, U., Mordmüller, B., Bacher, A., Fischer, M., Groll, M., Kurz, T.
J. Med. Chem., 2013, 56, 8151-8162.(http://pubs.acs.org/doi/pdf/10.1021/jm4012559)

45. Histone Deacetylase (HDAC) Inhibitors with a Novel Connecting Unit Linker Region Reveal a Selectivity Profile for HDAC4 and HDAC5 with Improved Activity against Chemoresistant Cancer Cells.
Marek L., Hamacher A., Hansen F.K., Kuna K., Gohlke H., Kassack M.U., Kurz T.
J. Med. Chem., 2013, 56, 427–436. (http://pubs.acs.org/doi/abs/10.1021/jm301254q)

44. α-Substituted β-Oxa Isosteres of Fosmidomycin: Synthesis and Biological Evaluation.
Brücher, K., Illarionov, B., Held, J., Tschan, S., Kunfermann, A., Pein, M. K., Bacher, A., Gräwert, T., Maes, L., Mordmüller, B., Fischer, M., Kurz, T.
J. Med. Chem., 2012, (55): 6566-6575. DOI: 10.1021/jm300652f. (http://pubs.acs.org/doi/pdf/10.1021/jm300652f)

43. Crystal Structure of Brucella abortus Deoxyxylulose-5-phosphate Reductoisomerase-like (DRL) Enzyme Involved in Isoprenoid Biosynthesis.
Pérez-Gil, J., Calisto, B. M., Behrendt, C., Kurz, T., Fita, I., Rodríguez-Concepción, M.
J. Biol. Chem., 2012, 287, 15803-15809. (http://www.jbc.org/content/287/19/15803.full.pdf+html)

42. Reverse Fosmidomycin Derivatives against the Antimalarial Drug Target IspC (Dxr).
Behrendt, C. T., Kunfermann, A., Illarionova, V., Matheeussen, A., Pein, M. K., Gräwert, T., Kaiser, J., Bacher, A., Eisenreich, W., Illarionov, B., Fischer, M., Maes L., Groll, M., Kurz T.
J. Med. Chem., 2011, 54, 6796-6802. (pubs.acs.org/doi/pdfplus/10.1021/jm200694q)

41. Synthesis and antimalarial activity of 4-alkylidene(arylidene)hydrazono-1,3-oxazinan-2-ones and 3-hydroxy-N'-alkylidene(arylidene)propanehydrazonamides.
Khankischpur, M., Kurz, T.
Aust. J. Chem., 2010, 63, 1430-1463.

40. Synthesis and antiplasmodial activity of highly active reverse analogs of the antimalarial drug candidate Fosmidomycin.
Behrendt, C. T., Kunfermann, A., Illarionova, V., Matheeussen, A., Gräwert, T., Groll, M., Rohdich, F., Bacher, A., Eisenreich, W., Fischer, M., Maes L., Kurz T.
ChemMedChem 2010, 5, 1673-1676. Highlighted in Nachrichten aus der Chemie.

39. Synthesis and reactivity of 4-aralkoxy(alkoxy)-5,6-dihydro-2H-1,3-oxazine-2-ones.
Kurz, T., Khankischpur, M.
Synthesis 2009, 4068-4074.

38. Microwave-Assisted Conversion of 4-Nitrophenyl Esters into O-protected Hydroxamic Acids.
Kurz, T., Pein, M. K., Marek, L., Behrendt, C. T., Spanier, L., Kuna, K., Brücher, K.
Eur. J. Org. Chem., 2009, 2939-2942.

37. Convenient Microwave-Assisted synthesis of 5-funktionalized 1,2,4-Triazolium ylides starting from N’,N’-Disubstituted Carbohydrazonamides.
Khankischpur, M., Kurz, T.
Eur. J. Org. Chem., 2008, 6029-6033 und Synfacts 2009, 2, 0144.

36. Microwave-assisted synthesis of 3-substituted 2-imino-pyrido[2,3-e][1,3]oxazin-4-ones.
Kurz, T., Pein, M.
Lett. Org. Chem. 2008, 599-601.

35. γ-Substituted Bis(pivaloyloxymethyl)ester Analogues of Fosmidomycin and FR900098.
Kurz, T., Behrendt, C., Pein, M., Kaula, U., Bergmann, B., Walter, R. D.
Archiv Pharm. 2007, 340, 661-666.

34. Conformationally Restrained Aromatic Analogues of Fosmidomycin and FR900098.
Kurz, T., Schlüter, K., Pein, M., Behrendt, C., Bergmann, B., Walter, R., D.
Archiv Pharm. 2007, 340, 339-344.

33. Synthesis of 3-Alkoxy-5,6-dihydro-4H-1,2,5-oxadiazines from Alkyl α-Amino-hydroximates.
Kurz, T., Thimann, W., Geffken, D.
Synthesis 2007, 1453-1455.

32. Rapid and efficient microwave-assisted synthesis of 5-Amino-3-aralkoxy(methoxy)amino-1,2,4-oxadiazoles.
Kurz, T., Lolak, N., Geffken, D.
Tetrahedron Lett., 2007, 48, 2233-2235.

31. α-Phenylethyl Substituted Bis(pivaloyloxmethyl)ester Analogues of Fosmidomycin and FR900098.
Kurz, T., Behrendt, C., Kaula, U., Bergmann, B., Walter, R. D.
Aust. J. Chem., 2007, 60, 154-158.

30. Arylmethyl substituted derivatives of Fosmidomycin: Synthesis and antimalarial activity.
Schlüter K., Walter, R. D., Bergmann, B., Kurz, T.
Eur. J. Med. Chem., 2006, 41, 1385-1397.

29. Synthesis of 1-Hydroxypyrrolidin-2,5-dione Derivatives of the Phosphonic-hydroxamic Acid Antibiotic SF-2312.
Owotoki, W., Geffken, D., Kurz, T.
Aust. J. Chem., 2006, 59, 283-288.

28. Rapid microwave assisted synthesis of 3-substituted 4-thioxo-oxazolidin-2-ones.
Kurz, T., Widyan, K., Khankischpur, M.
Tetrahedron Lett., 2006, 47, 4241-4243.

27. Synthesis and antimalarial activity of chain substituted pivaloyloxymethyl ester analogues of Fosmidomycin and FR900098.
Kurz, T., Schlüter K., Kaula, U., Bergmann, B., Walter, R. D., Geffken, D.
Bioorg. Med. Chem., 2006, 14, 5121-5135.

26. Microwave-assisted Base Catalysed Rearrangement of 3-Aryl(arylalkyl)-4-imino-oxazolidin-2-ones into 4-Arylimino- and 4-Arylalkylimino-oxazolidin-2-ones.
Kurz, T., Widyan, K., Khankischpur, M.
Synthesis 2006, 1803-1806.

25. Novel Synthesis of Fluorinated Cyanoketene N,S-Acetals and Their Conversion to Fluorinated Pyrazole Derivatives.
Kurz, T., Widyan, K., Elgemeie, G. H.
Phosphorus, Sulfur, and Silicon, 2006, 181, 299.

24. Preparation of 1,4-benzothiazepin-5-ones as antipsychotics.
Kurz, T., Geffken, D., Mesaros R.
(BioAgency AG), WO 2005/082873 A2, 2005.

23. Neue 1,4-Benzooxazepane oder 1,4-Benzothiazepane und Derivate.
Kurz, T., Geffken, D., Mesaros R.
(BioAgency AG), DE 102004010830 A1, 2005.

22. Phosphororganische Verbindungen und deren Verwendung.
Kurz, T., Geffken, D.; Kaula, U.
(BioAgency AG), DE 10356410 A1, 2005.

21. Organophosphoric compounds and use thereof.
Kurz, T., Geffken, D., Kaula, U.
(BioAgency AG), WO 2005/048715 A2, 2005.

20. AFMoC Enhances Predictivity of 3D QSAR: A Case Study with DOXP-reductoisomerase.
Silber, K., Heidler, P., Kurz, T., Klebe, G.
J. Med. Chem. 2005, 48, 3547-3563.

19. Microwave-assisted conversion of 3-substituted oxazolidin-2,4-diones into α-Hydroxyamides.
Kurz, T., Widyan, K.
Tetrahedron 2005, 61, 7247-7251.

18. Phosphororganische 4-Iminohydantoinderivate.
Kurz, T., Widyan, K., Geffken, D.
(BioAgency AG) DE 10337761 A1, 2005.

17. Preparation of organophosphoric 4-iminohydantoin derivatives useful as pharmaceutical or herbicidal agents.
Kurz, T., Widyan, K., Geffken, D.
(BioAgency AG) WO 2005/016942 A1, 2005.

16. Conventional and Microwave-Assisted Conversion of Substituted 3-Amino-oxazolidin-2,4-diones into N',N'-Disubstituted α-Hydroxyhydrazides.
Kurz, T., Widyan, K.
J. Org. Chem., 2005, 70, 3108-3112.

15. Synthesis of novel pyrido[2,3-e][1,3]oxazines.
Kurz, T.
Tetrahedron, 2005, 61, 3091-3096.

14. Synthesis of Novel 4-Functionalised Oxazolidin-2-ones.
Kurz, T., Widyan, K.
Synthesis, 2005, 1340-1344.

13. Efficient Conversion of O-Substituted 3-Hydroxy-4-imino-oxazolidin-2-ones into O-Substituted α-Hydroxyamidoximes.
Kurz, T., Widyan, K.
Org. Lett., 2004, 6, 4403-4405.

12. A convenient synthesis of 3-amino-4-imino(thioxo)-imidazolidin-2-ones.
Kurz, T., Widyan, K.
Tetrahedron Lett., 2004, 45, 7049-7051.

11. One-pot Synthesis of 4-Methoxy(aralkoxy)-imino-areno[1,3]oxazin-2-ones.
Kurz, T., Widyan, K., Wackendorff, C., Schlüter, K.
Synthesis, 2004, 1987-1990.

10. O-Protected 3-hydroxy-oxazolidin-2,4-diones: novel precursors in the synthesis of α-hydroxyhydroxamic acids.
Kurz, T., Widyan, K.
Org. Biomol. Chem., 2004, 2, 2023-2027.

9. Synthesis and reactivity of 3-aralkoxy-4-imino-imidazolidin-2-ones: a novel class of 4-iminohydantoins.
Kurz, T., Geffken, D., Widyan, K.
Tetrahedron, 2004, 60, 2409-2416.

8. Synthesis of 3-(3,5-Dioxo-[1,2,4]-oxadiazolidin-2-yl)propylphosphonic Acids.
Kurz, T., Geffken, D., Wackendorff, C.
Sci. Pharm., 2003, 71, 39-49.

7. Carboxylic Acid Analogues of Fosmidomycin.
Kurz, T., Geffken, D., Wackendorff, C.
Z. Naturforsch., 2003, 58b, 457-461.

6. Hydroxyurea Analogues of Fosmidomycin.
Kurz, T., Geffken, D., Wackendorff, C.
Z. Naturforsch., 2003, 58b, 106-110.

5. 5,5-Disubstituted thiazolidine derivatives pesticides.
Iwataki, I., Rudchenko, F., Kurz, T., Semer, C. R., Kucharek, T. A., Geffken, D.
US-Pat. (Nippon Soda Co., Ltd.), Patent No.:6,476,055 B1, Nov. 5, 2002, Patent No.:US 2003/0114649 A1, Jun. 19, 2003, Patent No.:6,713,629 B2, Mar. 30, 2004.

4. Regiospecific synthesis of 4-(2-oxoalkyl)pyridines.
Katritzky, A. R., Zhang, S., Kurz, T., Wang, M.
Org. Lett., 2001, 3, 2807-2809.

3. α-Benzotriazolylpyridines and their N-oxides.
Katritzky, A. R., Kurz, T., Zhang, S., Voronkov, M.
Heterocycles, 2001, 55, 1703-1710.

2. Cyclization of thiocyanato malonates with hydroxylamines to 5-carboxyalkyl-4-oxo-thiazoli(di)nes.
Kurz, T., Geffken, D.
Heterocycl. Commun., 1999, 5, 325-328.

1. Synthesis of 3-amino(alkoxy)-2,4-dioxo-1,3-oxazolidin-5-carboxylates from tartronic esters.
Kurz, T., Geffken, D.
Z. Naturforsch., 1999, 54b, 667-673.

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