Martin-Luther-Universität Halle-Wittenberg

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Publikationen

Publikationen

(1997 - 2014)

Veröffentlichungen

1.Kuckländer U., Hilgeroth A.:
Versuche zur Darstellung N-substituierter Dihydrpyridine nach Hantzsch.
Arch. Pharm. (Weinheim), 327, 287-294 (1994).
2.Hilgeroth A.:
Solid-state Synthesis of Novel 3,9-Diazatetraasteranes.
Chem. Letters, 1269-1270 (1997).
3.Hilgeroth A., Baumeister U., Heinemann F. W.:
Novel Solid-State Synthesis of Polyfunctionalized 3,9-Diazatetraasteranes.
Eur. J. Org. Chem., 1213-1218 (1998).
4.Hilgeroth A., Heinemann F. W.:
Novel solid-state synthesis of dimeric 4-aryl-1,4-dihydropyridines.
J. Heterocyclic Chem., 35, 359-364 (1998).
5.Hilgeroth A., Kuna K., Kuckländer U.:
Novel Functionalized 1,4,4a,9a-Tetrahydro-1-aza-9-oxafluorenes by Cycloaddition of 4-(4-Methoxyphenyl)-1,4-dihydropyridines and p-Benzoquinone, als Communication.
J. Heterocyclic Chem., 35, 551-553 (1998).
6.Hilgeroth A., Kuna K., Kuckländer U.:
Novel Synthesis Of Polyfunctionalized 1,4,4a,9a-Tetrahydro-1-aza-9-oxafluorenes By Unexpected Cycloaddition Of 4-(4-Methoxyphenyl)-1,4-dihydropyridines and p-Benzoquinone.
Heterocycles, 48, 1649-1658 (1998).
7.Hilgeroth A.:
HIV-1 Protease-Inhibitoren im Überblick.
Pharm. Uns. Zeit, 27, 22-25 (1998).
8.Hilgeroth A.:
Neue Nucleosidanaloga in der Therapie viraler Erkrankungen im Überblick.
Pharm. Uns. Zeit, 27, 111-116 (1998).
9.Hilgeroth A.:
Neue dimere 1,4-Dihydropyridine.
Deutsches Patent DE 197 56 881 (1998).
10.Hilgeroth A., Billich A.:
Cage Dimeric 4-Aryl-1,4-dihydropyridines as Promising Lead Structures for the Development of a Novel Class of HIV-1 Protease Inhibitors.
Arch. Pharm. Pharm. Med. Chem., 332, 3-5 (1999).
11.Hilgeroth A.:
Neue Zytostatika im Überblick.
Pharm. Uns. Zeit, 28, 309-313 (1999).
12.Hilgeroth A., Baumeister U., Heinemann F. W.:
Topochemical investigations of dimerizing 4-aryl-1,4-dihydropyridines by X-ray crystal structure analysis.
J. Mol. Structure, 474, 267-274 (1999).
13.Hilgeroth A., Fleischer R., Wiese M., Heinemann F. W.:
Comparison of azacyclic urea A-98881 as HIV-1 protease inhibitor with cage dimeric N-benzyl 4-(4-methoxyphenyl)-1,4-dihydropyridine as representative of a novel class of HIV-1 protease inhibitors: A molecular modeling study.
J. Comput.-Aided Mol. Design, 13, 233-242 (1999).
14.Hilgeroth A., Hempel G., Baumeister U., Reichert D.:
Solid-state photodimerization of 4-aryl-1,4-dihydropyridines studied by 13CPMAS NMR spectroscopy.
Solid State Nucl. Mag. Res., 13, 231-243 (1999).
15.Hilgeroth A., Hempel G., Baumeister U., Reichert D.:
Solid-state formation of centrosymmetric cage dimeric 4-aryl-1,4-dihydroypridines via non-symmetric syn-dimers studied by 13C cross-polarization magic angle spinning NMR spectroscopy.
Magn. Reson. Chem., 37, 376-381 (1999).
16.Hilgeroth A., Baumeister U., Heinemann F. W.:
Rotameric Properties Of Novel N-Acyl- and N-Acyloxy-Dimeric 4-Phenyl-1,4-dihydropyridines Derived From Developed Solid-State Synthesis.
Heterocycles, 51, 2367-2376 (1999).
17.Hilgeroth A., Billich A.:
Cage Dimeric N-Acyl- and N-Acyloxy-4-aryl-1,4-dihydropyridines as First Representatives of a Novel Class of HIV-1 Protease Inhibitors.
Arch. Pharm. Pharm. Med. Chem., 332, 380-384 (1999).
18.Hilgeroth A., Wiese M., Billich A.:
Synthesis and Biological Evaluation of First N-Alkyl Cage Dimeric 4-Aryl-1,4-dihydropyridines as Novel Nonpeptidic HIV-1 Protease Inhibitors.
J. Med. Chem., 42, 4729-4732 (1999).
19.Hilgeroth A., Langner A.:
First Bioanalytical Evaluation of Nonpeptidic Cage Dimeric HIV-1 Protease Inhibitor N-Benzyl 4-Aryl-1,4-dihydropyridine H17: Biotransformation and Toxicity on Hep G2 Cells.
Arch. Pharm. Pharm. Med. Chem., 333, 32-34 (2000).
20.Hilgeroth A., Baumeister U., Heinemann F. W.:
Solution-Dimerization of 4-Aryl-1,4-dihydropyridines.
Eur. J. Org. Chem., 245-249 (2000).
21.Hilgeroth A.:
Interaktionen als Schwerpunkt in der Pharmazeutischen Chemie.
Pharm. Ztg., 145, 100 (2000).
22.Hilgeroth A., Baumeister U.:
Erste funktionalisierte 6,12-Diazatetrakishomocubane.
Angew. Chem., 112, 588-590 (2000).
The First Functionalized 6,12-Diazatetrakishomocubanes.
Angew. Chem. Int. Ed., 39, 576-578 (2000).
23.Hilgeroth A., Langner A.:
Bioanalysis of Syn-dimeric N-Benzyl 4-Aryl-1,4-dihydropyridine H19: Metabolic and Cytotoxic Properties in Hep G2 Cells.
Arch. Pharm. Pharm. Med. Chem., 333, 195-197 (2000).
24.Hilgeroth A., Langner A.:
Plasma Protein Binding Properties of Dimeric 4-Aryl-1,4-dihydropyridines as Novel Nonpeptidic HIV-1 Protease Inhibitors.
Pharmazie, 55, 542-543 (2000).
25.Hilgeroth A., Dressler C., Neuhoff S., Langguth P., Spahn-Langguth H.:
Dimeric 4-aryl-1,4-dihydropyridines as novel HIV-1 protease inhibitors - affinities to intestinal P-glycoprotein.
Pharmazie, 55, 784-785 (2000).
26.Hilgeroth A., Brachwitz K., Baumeister U.:
Regioselective Formation Of Novel Functionalized 1-Aza-9-oxafluorenes.
Heterocycles, 55, 661-669 (2001).
27.Hilgeroth A., Wollmann J.:
HIV-Forschung - In der dritten Dekade einer Odyssee.
Pharm. Ztg., 146, 2632-2636 (2001).
28.Hilgeroth A.:
Neue Molekülklassen von HIV-1 Proteaseinhibitoren?
Pharm. Uns. Zeit, 30, 213-216 (2001).
29.Hilgeroth A., Billich A., Lilie H.:
Synthesis and biological evaluation of first N-alkyl syn dimeric 4-aryl-1,4-dihydropyridines as competitive HIV-1 protease inhibitors.
Eur. J. Med. Chem., 36, 367-374 (2001).
30.Hilgeroth A., Baumeister U.:
Formation of Novel Photodimers from 4-Aryl-1,4-dihydropyridines.
Chem. Eur. J., 7, 4599-4603 (2001).
31.Brachwitz K., Hilgeroth A.:
Synthesis and First Biological Evaluation of 1-Aza-9-oxafluorenes as Novel Lead Structures for the Development of Small-sized Cytostatics.
Biorg. Med. Chem. Lett., 12, 411-413 (2002).
32.Hilgeroth A., Tykarska E., Jaskolski M.:
Crystal structure of a novel synthetic inhibitor of HIV-1 protease.
J. Mol. Structure, 605, 63-70 (2002).
33.Hilgeroth A., Heinemann F. W., Baumeister U.:
First Rotameric Anti Dimers and 3,9-Diazatetraasteranes From Unsymmetrically Substituted N-Acyl and N-Acyloxy-4-aryl-1,4-dihydropyridines.
Heterocycles, 57, 1003-1016 (2002).
34.Hilgeroth A.:
Dimeric 4-Aryl-1,4-dihydropyridines: Development of a Third Class of Nonpeptidic HIV-1 Protease Inhibitors.
Min. Rev. Med. Chem., 2, 235-247 (2002).
35.Hilgeroth A., Molnár J., De Clercq E.:
Mit molekularer Symmetrie zu neuen Wirkstoffen: Hydroxymethyl-substituierte 3,9-Diazatetraasterane als erste eigenständige Klasse symmetrischer MDR-Modulatoren, Angew. Chem., 114, 3772-3775 (2002).
Using Molecular Symmetry to Form New Drugs: Hydroxymethyl-substituted 3,9-Diazatetraasteranes as the First Class of Symmetric MDR Modulators.
Angew. Chem. Int. Ed., 41, 3623-3625 (2002).
36.Brachwitz K., Voigt B., Meijer L., Lozach O., Schächtele C., Molnár J., Hilgeroth A.:
Evaluation of The First Cytostatically Active 1-Aza-9-oxafluorenes as Novel Selective CDK1-Inhibitors with P-Glycoprotein Modulating Properties.
J. Med. Chem., 46, 876-879 (2003).
37.Hilgeroth A., Lilie H.:
Structure-activity relationships of first bishydroxymethyl-substituted cage dimeric 4-aryl-1,4-dihydropyridines as HIV-1 protease inhibitors.
Eur. J. Med. Chem., 38, 495-499 (2003).
38.Voigt B., Hilgeroth A.:
3-Hydroquinolyl-quinolines and Bisquinolyl-anelated Oxepin as Reaction Products From p-Benzoquinone and N-Acetyl-1,4-dihydroquinolines.
Heterocycles, 60, 2223-2230 (2003).
39.Richter M., Gyémánt N., Molnár J., Hilgeroth A.:
Comparative Effects on Intestinal Absorption in Situ by P-Glycoprotein Modifying HIV Protease Inhibitors.
Pharm. Res., 21, 1862-1866 (2004).
40.Voigt B., Meijer L., Lozach O., Schächtele C., Totzke F., Hilgeroth A.:
Novel CDK-Inhibition Profiles of Structurally Varied 1-Aza-9-oxafluorenes.
Bioorg. Med. Chem. Letters, 15, 823-825 (2005).
41.Sharples D., Spengler G., Molnár J, Antal Z., Molnár A., Kiss J., Szabó A., Hilgeroth A., Gallo S., Mahamoud A., Barbe J.:
The interaction between resistance modifiers such as pyrido[3,2-g]quinoline, azafluorene and pregnane derivatives with DNA, plasmid DNA and tRNA.
Eur. J. Med. Chem., 40, 195-202 (2005).
42.Wollmann J., Baumeister U., Hilgeroth A.:
Topochemical characterization of photostable 4-hydroxyaryl-1,4-dihydropyridines by X-ray crystal structure analysis.
J. Mol. Structure, 743, 169-175 (2005).
43.Wollmann J., Richter M., Molnár J., Hilgeroth A.:
First Insight in Symmetry and Flexibilty of Membrane Efflux Pump P-glycoprotein by Novel Bifunctional Modulators.
ChemBioChem., 8, 1353-1356 (2005).
44.Hilgeroth A., Molnár A., Molnár J., Voigt B.:
Correlation of Calculated Molecular Orbital Energies of Some Phenothiazine Compounds with MDR-Reversing Properties.
Eur. J. Med. Chem., 41, 548-551 (2006).
45.Richter M., Molnár J., Hilgeroth A.:
Biological Evaluation of Bishydroxymethyl Substituted Cage Dimeric 1,4-Dihydroypyridines as Novel Class of P-Glycoprotein Modulating Agents in Cancer Cells.
J. Med. Chem., 49, 2838-2840 (2006).
46.Hilgeroth A.:
Neue bifunktionale dimere 1,4-Dihydropyridine.
Deutsches Patent DE 10/2004/037/885 (2006).
47.Hilgeroth A.:
Neue gemischte dimere 1,4-Dihydropyridine.
Deutsches Patent DE 10/2004/037/911 (2006).
48.Wollmann J., Molnár J., Hilgeroth A.:
Physicochemical Characteristics Of Novel P-Glycoprotein Inhibitors Of The Cage Dimeric 1,4-Dihydropyridine Type.
Med. Chem., 2, 565-568 (2006).
49.Richter M., Gyémánt N., Molnár J., Hilgeroth A.:
P-Glycoprotein Effects of Cyclic Urea HIV Protease Inhibitor DMP 323 in Competitional Absorption Studies.
Arch. Pharm. Chem. Life Sci., 339, 625-628 (2006).
50.Wollmann J., Hilgeroth A.:
Antiretrovirale Therapie: Neue Ansätze im Kampf gegen HIV.
Pharm. Ztg., 151, 4496-4503 (2006).
51.Voigt B., Coburger C., Molnár J., Hilgeroth A.:
Structure-activity relationships of novel N-acyloxy-1,4-dihydropyridines as P-glycoprotein inhibitors.
Bioorg. Med. Chem., 15, 5110-5113 (2007).
52.Voigt B., Krug M., Schächtele C., Totzke F., Hilgeroth A.:
Probing Novel 1-Aza-9-oxafluorenes as Selective GSK-3ß Inhibitors.
ChemMedChem, 3, 120-126 (2008).
53.Wollmann J., Baumert C., Erlenkamp G., Sippl W., Hilgeroth A.:
Novel Insight in Inhibitor Binding of Highly Symmetric HIV-1 Protease.
ChemBioChem, 9, 874-878 (2008).
54.Coburger C., Wollmann J., Baumert C., Krug M., Molnár J., Hilgeroth A.:
Novel Insight in SAR and Bioanalysis of P-Glycoprotein Targeting Highly Potent Tetrakishydroxymethyl Substituted 3,9-Diazatetrasteranes.
J. Med. Chem., 51, 5871-5874 (2008).
55.Duarte N., Járdánházy A., Molnár J., Hilgeroth A., Ferreira M.-J. U.:
Synergistic interaction between p-glycoprotein modulators and epirubicin on resistant cancer cells. Bioorg. Med. Chem., 16, 9323-9330 (2008).
56.Krug M., Hilgeroth A.:
Recent Advances in the Development of Multi-Kinase Inhibitors.
Min. Rev. Med. Chem., 8, 1312-1327 (2008).
57.Richter M., Richter A., Langner A., Hilgeroth A.:
Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps.
Eur. J. Med. Chem., 44, 3060-3063 (2009).
58.Coburger C., Lage H., Molnár J., Hilgeroth A.:
Impact of Novel MDR Modulators on Human Cancer Cells: Activities and Induction Studies.
Pharm. Res., 26, 182-187 (2009).
59.Baumert C., Hilgeroth A.:
Recent Advances in the Development of P-gp Inhibitors.
Anti-Cancer Agents Med. Chem., 9, 415-436 (2009).
60.Lage H., Duarte N., Coburger C., Hilgeroth A., Ferreira M.-J. U.:
Antitumor activity of terpenoids against classical and atypical multidrug resistant cancer cells.
Phytomedicine, 17, 441-448 (2010).
61.Krug M., Voigt B., Baumert C., Lüpken R., Molnár J., Hilgeroth A.:
First Biological Evaluation of Developed 3-Benzyloxyfluorenes as Novel Class of MDR Modulators.
Eur. J. Med. Chem., 45, 2683-2688 (2010).
62.Coburger C., Lage H., Molnár J., Langner A., Hilgeroth A.:
MDR reversal properties and cytotoxic evaluation of representatives of a novel class of HIV-1 protease inhibitors.
J. Pharm. Pharmacol., 62, 1704-1710 (2010).
63.Coburger C., Wollmann J., Krug M., Baumert C., Seifert M., Molnár J., Lage H., Hilgeroth A.:
Novel structure-activity relationships and selectivity profiling of novel cage dimeric 1,4-dihydropyridines as multidrug resistance (MDR) modulators.
Bioorg. Med. Chem., 18, 4983-4990 (2010).
64.Krug M., Erlenkamp G., Sippl W., Schächtele C., Totzke F., Hilgeroth A.:
Discovery and selectivity profiling of 4-benzylamino 1-aza-9-oxafluorene derivatives as lead structures for IGF-1R inhibitors, Bioorg. Med. Chem. Letters, 20, 6915-6919 (2010).
65.Krawczyk S., Coburger C., Hilgeroth A.:
HIV-Infektion: Hoffnung auf neue Therapien, Pharm. Ztg., 155, 3999-4107 (2010).
66.Krug M., Wichapong K., Erlenkamp G., Sippl W., Schächtele C., Totzke F., Hilgeroth A.:
Discovery of 4-Benzylamino Substituted α-Carbolines as a Novel Class of Receptor Tyrosine Kinase Inhibitors, ChemMedChem, 6, 63-72 (2011).
67.Telep El-Sayed M., Abbas M., Hilgeroth A.:
Efficient One-Pot Formation of Substituted γ-Amino Acids,
Letters Org. Chem., 8, 320-324 (2011)
68.Tell V., Hilgeroth A.:
Alzheimer Demenz: Neue Arzneistoffe, neue Hoffnung?,
Pharm. Ztg., 156, 3900-3906 (2011).
69.Krawczyk S., Otto M., Otto A., Coburger C., Krug M., Seifert M., Tell V., Molnár J., Hilgeroth A.:
Discovery of pyridine-2-ones as novel class of multidrug resistance (MDR) modulators: First structure-activity relationships,
Bioorg. Med. Chem., 19, 6309-6315 (2011).
70.Hilgeroth A., Hemmer M., Coburger C.:
The Impact of the Induction of Multidrug Resistance Transporters in Therapies by Used Drugs: Recent Studies,
Mini Rev. Med. Chem., 12, 1127-1134 (2012).
71.Tell V., Holzer M., Herrmann L., Mahmoud K. A., Schächtele C., Totzke F., Hilgeroth A.:
Multitargeted Drug Development: Discovery and Profiling of Dihydroxy Substituted 1-Aza-9-oxafluorenes as Lead Compounds Targeting Alzheimer Disease Relevant Kinases,
Bioorg. Med. Chem. Letters, 22, 6914-6918 (2012).
72.Tell V., Mahmoud K., Wichapong K., Schächtele C., Totzke F., Sippl W., Hilgeroth A.:
Novel aspects in structure-activity relationships of profiled 1-aza-9-oxafluorenes as inhibitors of Alzheimer´s disease relevant kinases cdk1, cdk5 and gsk3β,
Med. Chem. Commun., 3, 1413-1418 (2012).
73.Baumert C., Günthel M., Krawczyk S., Hemmer M., Wersig T., Langner A., Molnár J., Lage H., Hilgeroth A.:
Development of Small-Molecule P-gp Inhibitors of the N-Benzyl 1,4-Dihydropyridine Type: Novel Aspects in SAR and Bioanalytical Evaluation of Multidrug Resistance (MDR) Reversal Properties,
Bioorg. Med. Chem., 21, 166-177 (2013).
74.Telep El-Sayed M., Mahmoud K., Hilgeroth A.:
Synthesis of β-Nitroamines via Classical Mannich and Aza-Henry Reactions,
Curr. Org. Chem., 17, 1200-1224 (2013).
75.Hilgeroth A., Baumert C., Coburger C., Seifert M., Krawczyk S., Hempel C., Krug M., Molnár J., Lage H.:
Novel Structurally Varied N-Alkyl 1,4-Dihydropyridines as ABCB1 Inhibitors: Structure-Activity Relationships, Biological Activity and First Bioanalytical Evaluation,
Med. Chem., 9, 487-493 (2013).
76.Tell V., Hilgeroth A.:
Recent developments of protein kinase inhibitors as potential AD therapeutics,
Frontiers Cell. Neurosci., 7, doi: 10.3389/fncel.2013.00189  (2013).
77.El-Sayed M., Mahmoud K., Hilgeroth A.:
Glacial acetic acid as efficient catalyst for simple synthesis of diindolylmethanes,
Curr. Chem. Letters, 3, 7-14 (2014).
78.Mahmoud K. A., Krug M., Wersig T., Slynko I., Schächtele C., Totzke F., Sippl W., Hilgeroth A.:
Discovery of 4-anilino α-carbolines as novel Brk inhibitors,
Bioorg. Med. Chem. Letters, 24, 1948-1951 (2014).
79.Hilgeroth A., Tell V., Kramer S., Totzke F., Schächtele C.:
Approaches to a Multitargeting Drug Development: First Profiled 3-Ethoxycarbonyl-1-aza-9-oxafluorenes Representing a Perspective Compound Class Targeting Alzheimer Disease Relevant Kinases CDK1, CDK5 and GSK-3β,
Med. Chem., 10, 90-97 (2014).
80.Mahmoud K. A., Wersig T., Slynko I., Totzke F., Schächtele C., Oelze, M., Sippl W., Ritter C., Hilgeroth A.:
Novel inhibitors of breast cancer relevant kinases Brk and HER2,
Med. Chem. Commun., 5, 659-664 (2014).
81.Krawczyk S., Hilgeroth A.:
HIV-1-Reverse-Transkriptase-Inhibitoren,
Pharmakon, 2, 270-276 (2014).

Buch-Beiträge

1.Hilgeroth A.:
Recent advances in the solid-state photochemistry of 1,4-dihydropyridines. In: Recent Res. Devel. Pure & Applied Chemistry, Vol. 3. Editor: S. G. Pandalai, Transworld Research Network, Trivandrum (India), pp. 153-159.

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