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2006
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Neuhaus W, Lauer R, Oelzant
S, Fringeli UP, Ecker GF, Noe CR: "A novel flow based
hollow-fiber blood-brain barrier in vitro model with immortalised
cell line PBMEC/C1-2". J Biotechnol 125, 127-141 (2006)
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Chiba P, Ecker GF, Kopp
S, Mihalek I, Lichtarge O. "Role of transmembrane domain/transmembrane
domain interfaces of P-glycoprotein (ABCB1) in solute transport.
Convergent information from photoaffinity labeling, site directed
mutagenesis and in silico importance preddiction"
, Curr Med Chem 13, 793-805 (2006)
2005
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D. Kaiser, M. Smiesko, S.
Kopp, P. Chiba, G.F. Ecker: "Interaction field based
and hologram based QSAR analysis of propafenone-type modulators
of multidrug resistance", Med. Chem. 1: 431-444 (2005).
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D. Kaiser, B. Zdrazil, G.F.
Ecker: "Similarity based descriptors (SIBAR) - a tool
for safe exchange of chemical information?", J. Comput.-Aided
Mol. Design, in press
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K. Pleban, D. Kaiser, S.
Kopp, M. Peer, P. Chiba, G.F. Ecker: "Targeting drug-efflux
pumps - a pharmacoinformatic approach", Acta Biochim.
Polon. 52: 737-740 (2005).
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G. F. Ecker: "In
silico screening of promiscuous targets and antitargets",
Chemistry Today 23: 39-42 (2005).
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K. Pleban, G.F. Ecker: "Inhibitors
of P-glycoprotein: Lead identification and optimisation",
Minirev. Med. Chem. 5: 153-165 (2005).
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G. F. Ecker, K. Pleban,
S. Kopp, E. Csaszar, G. J. Poelarends, M. Putman, D. Kaiser, W.
N. Konings, P. Chiba: “A three dimensional model for
the substrate binding domain of the multidrug ABC transporter
LmrA”, Mol. Pharmacol.67: 365-374 (2005).
2004
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K. Pleban, A. Macchiarulo,
G. Costantino, R. Pellicciari, P. Chiba, G.F. Ecker: “Homology
model of the multidrug transporter LmrA from Lactococcus lactis”,
Bioorg. Med. Chem. Lett. 14, 5823-5826 (2004)
- M. Murias, N. Handler, T. Erker, K. Pleban,
G. Ecker, P. Saiko, T. Szekeres, W. Jäger: “Resveratrol
analogues as selective cyclooxygenase-2 inhibitors: synthesis and structure-activity
relationship”, Bioorg. Med. Chem. 12, 5571-5578 (2004)
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A. Macchiarulo, G. Costantino,
M. Meniconi, K. Pleban, G. Ecker, D. Bellocchi, R. Pellicciari: “Insights
into phenylalanine derivatives recognition of VLA-4 integrin: from
a pharmacophoric study to 3D-QSAR and molecular docking analyses”,
J. Chem. Inf. Comput. Sci., published online on July, 22 (2004)
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G.F. Ecker, P. Chiba: "Development
of modulators of multidrug resistance - a pharmacoinformatic approach",
J. Pure Appl. Chem. 76, 997-1005 (2004).
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K. Pleban, C. Hoffer, S. Kopp,
M. Peer, P. Chiba, G.F. Ecker: "Intramolecular distribution
of hydrophobicity influences pharmacological activity of propafenone-type
MDR modulators", Arch. Pharm. Pharm. Med. Chem. 337, 328-334
(2004).
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T. Langer, M. Eder, R.D. Hoffmann,
P. Chiba, G.F. Ecker: “Lead identification for modulators
of multidrug resistance based on in silico screening with a pharmacophoric
feature model”, Arch. Pharm. Pharm. Med. Chem. 337, 317-327
(2004).
- G.F. Ecker, C.R. Noe: "In silico prediction
models for blood-brain barrier permeation", Curr. Med. Chem.
11, 1617-1628 (2004).
- G.F. Ecker, P. Chiba: "Inhibitors of
ABC-type Drug Efflux Pumps - an overview on the actual patent situation",
Exp. Opin. Therapeutic Patents 14: 499-508 (2004).
- R. Bauer, R. Lauer, B. Linz, F. Pittner, G.
Peschek, G. Ecker, P. Friedl, C.R. Noe: "Development of an
in vitro blood brain barrier model based on immortalized porcine brain
microvascular endothelial cells", Il Farmaco 59, 133-137 (2004).
- C.T. Klein, D. Kaiser, G. Ecker: "Topological
distance based 3D descriptors for use in QSAR and diversity analysis",
J. Chem. Inf. Comput. Sci. 44, 200-209 (2004)
2003
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M. Schuetzer-Muehlbauer, B.
Willinger, R. Egner, G. Ecker, K. Kuchler: “Reversal of
antifungal resistance mediated by ABC efflux pumps from Candida albicans
functionally expressed in yeast”, Int. J. Antimicrobial
Agents 22: 291-300 (2003)
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D. Schmid, D.L. Staudacher,
H.G. Löw, P.G. Spieckermann, G.F. Ecker, S. Kopp, P. Chiba: “A
subset of highly effective propafenone-type MDR-modulators lacks effects
on cardiac action potential and mechanical twitch parameters of rat
papillary muscles”, J Pharmacol. Exp. Ther. 307: 589-596
(2003)
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G. Klopman, H. Zhu, G.F. Ecker,
P. Chiba: “Structure-Activity study of the multidrug resistance
reversal activity of propafenones”, J. Comp. Aided Molecular
Design 17: 291-297
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S. Rebitzer, D. Annibali, S.
Kopp, M. Eder, T. Langer, P. Chiba, G.F. Ecker, C.R. Noe: "In
silico sreening with benzofurane- and benzopyrane-type MDR-modulators",
Il Farmaco 58: 185-191 (2003)
2002
- C. Klein, D. Kaiser, S. Kopp, P. Chiba, G.F.
Ecker: "Similarity based SAR (SIBAR) as tool for early ADME
profiling", J. Comput. Aided Molecular Drug Design 16: 785-793
- R. Bauer, R. Lauer, B. Linz, F. Pittner, G.A.
Peschek, G.F. Ecker, P. Friedel, C.R. Noe: "An in vitro model
for blood brain barrier permeation", Sci. Pharm. 70: 317-324
(2002)
- P. Chiba, Th. Erker, M. Galanski, M. Hitzler,
G.F. Ecker: "Synthesis and multidrug-resistance modulating
activity of a series of thienothiazines", Arch. Pharm. Pharm.
Med. Chem. 335: 223-228 (2002)
- G.F. Ecker, E. Csaszar, S. Kopp, B. Plagens,
W. Holzer, W. Ernst, P. Chiba: "Identification of ligand-binding
regions of P-glycoprotein by activated-pharmacophore photoaffinity labeling
and MALDI-TOF mass spectrometry", Mol. Pharmacol. 61: 637-648
(2002)
- G.F. Ecker: "EUFEPS 2002 - New Safe
Medicines Faster", IDrugs 5, 1134-1137 (2002)· G.F.
Ecker: "Troxacitabine", Current Opinion in Investigational
Drugs 3, 1533-1538 (2002)
2001
- G. Ecker, P. Chiba: "Design and development
of propafenone-type inhibitors of drug efflux pumps", Recent
Res. Devel. Medicinal Chem. 1, 121-137 (2001)
- B. Wailzer, J. Klocker, G. Buchbauer, G. Ecker,
P. Wolschann: "Prediction of the aroma quality and the threshold
values of some pyrazines using artificial neural networks",
J. Med. Chem. 44, 2805-2813 (2001)
- G. Ecker, H. Kalchhauser, L. Lawtrakul, P.
Wolschann: "Levcromakalim revisited: NMR spectroscopic and
theoretical investigations", Monatsh. Chemie 132, 373-386
(2001)
- G.F. Ecker: "Linking genomic information
with drug design", IDrugs 4, 1114-1115 (2001)
2000
- H.-P. Buchstaller, C.D. Siebert, R.H. Lyssy,
G. Ecker, M. Krug, M.L. Berger, R. Gottschlich, C.R. Noe: “Thieno[2,3-b]pyridones
as Antagonists on the Glycine Site of the N-methyl-D-aspartate Receptor
– Binding Studies, Molecular Modeling and Structure-Activity-Relationships”,
Sci. Pharm. 68, 3-14 (2000)
- D. Kaiser, C. Tmej, P. Chiba, K.-J. Schaper,
G. Ecker: “Artificial Neural Networks in Drug Design II: Influence
of Learning Rate and Momentum Factor on the Predictive Ability”,
Sci. Pharm. 68, 57-64 (2000)
- D. Annibali, G. Ecker, W. Fleischhacker, T.
Helml, W. Holzer, C.R. Noe: “A Method for the Synthesis of
2,3-Disubstituted 2,3-Dihydrobenzofuranes”, Monatsh. Chemie
131, 375-382 (2000)
- G. Ecker: "New agent design and action",
IDrugs 3, 712-713 (2000)
- G. Ecker: „Apicularene A and B“,
Exp. Opin. Ther. Patents 10, 497-499 (2000)
- G. Ecker, T. Langer, P. Chiba: „Design
and Development of new Inhibitors of Drug Efflux Pumps“,
Proceedings of the 4th Annual National Symposium on Computational Science
and Engineering, March 27-29, 2000; p. 4-14
1999
- C. Tmej, P. Chiba, K.-J. Schaper, G. Ecker,
W. Fleischhacker: "Artificial Neural Networks as Versatile
Tools for Prediction of MDR-Modulatory Activity", Adv. Exp.
Med. Biol. 457, 95-105 (1999)
- G. Ecker: “Patent focus on agents
for tumour therapy: May – October 1999”, Exp. Opin.
Ther. Patents 9, 1627-1639 (1999)
- G. Ecker, M. Huber, D. Schmid, P. Chiba: "The
Importance of a Nitrogen Atom in Modulators of Multidrug Resistance",
Mol. Pharmacol. 56, 791-796 (1999)
- R. Hiessböck, C. Wolf, E. Richter, M.
Hitzler, P. Chiba, M. Kratzel, G. Ecker: "Synthesis and Multidrug
Resistance Modulating Activity of a Series of Dihydrobenzopyrans and
Tetrahydroquinolines", J. Med. Chem. 42, 1921-1926 (1999)
- D. Schmid, G. Ecker, E. Richter, M. Hitzler,
P. Chiba: "Structure-Activity Relationship Studies of Propafenone
Analogs based on P-Glycoprotein ATPase Activity Measurements",
Biochem. Pharmacol. 58, 1447-1456 (1999)
- G.Ecker: “KRN-2391“, Current
Opinion in Cardiovascular, Pulmonary & Renal Investigational Drugs
1, 619-629 (1999)
- G. Ecker: “Drug transport pumps:
from molecular biology and pharmacology to clinical implications“,
IDrugs 2, 1256-1257 (1999)
- G. Ecker: "Onconase", Curr.
Oppin. Oncologic, Endocrine & Metabolic Invest. Drugs 1, 229-236
(1999)
1998
- M. Spatzenegger, G. Ecker, W. Jäger: "Metabolism
of the new MDR-Modifier AM05 by Human Liver Microsomes", Sci.
Pharm. 66, 159-168 (1998)
- M. Salem, E. Richter, M. Hitzler, P. Chiba,
G. Ecker: "Studies on Propafenone-Type Modulators of Multidrug
Resistance VIII: Synthesis and Pharmacological Activity of Indanone
Analogues", Sci. Pharm. 66, 147-158 (1998)
- C. Tmej, P. Chiba, M. Huber, E. Richter, M.
Hitzler, K.-J. Schaper, G. Ecker: "A Combined Hansch/Free-Wilson
Approach as Predictive Tool in QSAR Studies on Propafenone-Type Modulators
of Multidrug Resistance", Arch. Pharm. Pharm. Med. Chem. 331,
233-240 (1998)
- P. Chiba, W. Holzer, M. Landau, G. Bechmann,
K. Lorenz, B Plagens, M. Hitzler, E. Richter, G. Ecker: "Substituted
4-Acylpyrazoles and -Pyrazolones: Synthesis and MDR-Modulating Activity",
J. Med. Chem. 41, 4001-4011 (1998)
- G. Ecker, W. Fleischhacker, C. Wolf, P. Weiß-Greiler,
P. Wolschan: "A Quantum Chemical Study of Levcromakalim",
Monatsh. Chemie 129, 633-642 (1998)
- P. Chiba, S. Rebitzer, E. Richter, M. Hitzler,
G. Ecker: "Synthesis and Pharmacological Activity of the Stereoisomeres
of GP-88, a Propafenone-type Modulator of Multidrug Resistance",
Bioorg. Med. Chem. Lett. 8, 829-832 (1998)
- P. Chiba, D. Annibali, M. Hitzler, E. Richter,
G. Ecker: "Studies on Propafenone-type Modulators of Multidrug
Resistance, VI: Synthesis and Pharmacological Activity of Compounds
with Varied Spacer Length between the Central Aromatic Ring and the
Nitrogen Atom", Il Farmaco 53 (5), 357-364 (1998)
- G. Riehs, G. Ecker, E. Urban: "Studies
on the Absolute Configuration and the Enantiomeric Purity of the Antibiotic
Heptelidic Acid", Sci. Pharm. 66, 199-204 (1998)
- G. Ecker: "Ion channels and proteinase
inhibition", IDrugs 1 (8), 870-872 (1998)
1997
- G. Ecker, T. Helml: "Sodium Channel
Modulators in Preclinical and Early Clinical Development",
Ion Channel Modulators 2, 584-591 (1997)
- I. Tumova, E. Racanska, J. Csöllei, G.
Ecker, R. Otrusnik, P. Svec: "Pharmacological-Toxicological
Evaluation of Some Newly Synthesized Analogues of Propafenone",
(tschech.) Ces. Slov. Farm. 46, 133-136 (1997)
- P. Chiba, B. Tell, W. Jäger, M. Spatzenegger,
E. Richter, M. Hitzler, G. Ecker: "Studies on Propafenone-type
Modulators of Multidrug-Resistance IV: Synthesis and Pharmacologic Activity
of 5-Hydroxy- and 5-Benzyloxy-Derivatives", Arch. Pharm.,
Pharm. Med. Chem. 330, 343-347 (1997)
- G. Ecker, P. Chiba: "Recent developments
in overcoming tumour cell multi-drug resistance", Exp. Opin.
Ther. Patents 7, 589-599 (1997)
- P. Chiba, M. Hitzler, E. Richter, M. Huber,
C. Tmej, G. Ecker: "Studies on Propafenone-type Modulators
of Multidrug Resistance III: Variations on the Nitrogen",
Quant. Struct.-Act. Rel. 16, 361-366 (1997)
- G. Ecker, C.R. Noe, W. Fleischhacker: "Improved
Synthesis of the Enantiomers of Propafenone using Chiral Building Blocks",
Monatshefte Chemie 128, 53-39 (1997)
- G. Ecker, P. Chiba, K.-J. Schaper: "Estimation
of Chemosensitizing Activity of Modulators of Multidrug Resistance via
Combined Simultaneous Analysis of Sigmoidal Dose-Response Curves",
J. Pharm. Pharmacol. 49, 305-309 (1997)
1996
- C. Wolf, P. Weiß-Greiler, P. Wolschan,
G. Ecker, W. Fleischhacker: "Synthesis and Conformational Analysis
of a Series of 1-Benzopyrano[3,4-b][1,4]oxazines Structurally Related
to Cromakalim", Die Pharmazie 51, 836-839 (1996)
- S. Prets, A. Jungreithmair, P. Chiba, G. Ecker:
"Comparison of Different Methods for Estimation of Lipophilicity
of Propafenone-Type Modulators of Multidrug Resistance", Sci.
Pharm. 64, 627-636 (1996)
- G. Ecker, P. Chiba, M. Hitzler, D. Schmid,
K. Visser, H.P. Cordes, J. Csöllei, J.K. Seydel, K.-J. Schaper:
"Structure-Activity Relationship Studies on Benzofurane Analogs
of Propafenone-Type Modulators of Tumor Cell Multidrug Resistance",
J. Med. Chem. 39 (24), 4767-4774 (1996)
- G. Ecker, E. Mohr, R. Geyer, W. Fleischhacker:
"Enantioseparation of Propafenone-Type Modulators of Multidrug-Resistance
on Cyclodextrin Based Chiral Stationary Phases", Sci. Pharm.
64, 1-11 (1996)
- M. Spatzenegger, G. Ecker, W. Jäger: "Determination
of the new MDR-modifier PFP 6 and its metabolites in human liver microsomes
by high performance liquid chromatography", Biomed. Chromatogr.
10, 127-130 (1996)
- P. Chiba, G. Ecker, D. Schmid, J. Drach, B.
Tell, S. Goldenberg, V.Gekeler: "Structural Requirements for
Activity of Propafenone Type Modulators in PGP-Mediated Multidrug Resistance",
Mol. Pharmacol. 49, 1122-1130 (1996)
1995
- G. Ecker, P. Chiba: "Structure-Activity-Relationship
Studies on Modulators of the Multidrug Transporter P-Glycoprotein -
an Overview", Wien. Klin. Wochenschr. 107, 681-686 (1995)
- C. Studenik, R. Lemmens-Gruber, P. Heistracher,
G. Ecker, A. Maxl, W. Fleischhacker: "Electromechanical Effects
of newly synthetized Propafenone Derivatives on isolated Guinea Pig
Heart Mucle Preparations", Arzneim. Forsch. 46, 134-138 (1996)
- P. Chiba, S. Burghofer, E. Richter, B. Tell,
A. Moser, G. Ecker: "Synthesis, Pharmacologic Activity and
Structure-Activity-Relationships of a Series of Propafenone-Related
Modulators of Multi-Drug-Resistance", J. Med. Chem. 38, 2789-2793
(1995)
- G. Ecker, W. Fleischhacker, T. Helml, C.R.
Noe, C. Studenik, B. Schade, P. Heistracher: "Synthese und
pharmakodynamische Aktivität von 2-(3-(2-Phenylethyl)benzofuran-2-yl)-N-propyl-ethanamin",
Arch. Pharm. 328, 343-348 (1995)
1994
- I. Tumova, E. Racanska, P. Svec, J. Csöllei,
G. Ecker: "Preparation and Pharmacological Profile of some
newly synthesized Analogues of Propafenone" (tschech.), Ces.
a Slov. Farm. 43, 229-232 (1994)
- G. Ecker, W. Fleischhacker, C.R. Noe: "New
Benzofurane-Type Antiarrhythmic Compounds Related to Propafenone",
Heterocycles 38, 1247-1256 (1994)
- G. Ecker, W. Fleischhacker, C.R. Noe: "Ein
Verfahren zur Synthese der Enantiomere von Propafenon", Arch.
Pharm. 327, 691-695 (1994)
- G. Ecker, W. Fleischhacker, T. Helml, C.R.
Noe, S. Scasny, R. Lemmens-Gruber, C. Studenik, H. Marei, P. Heistracher:
"Improved Synthesis and Pharmacologic Activity of the Enantiomers
of a New Benzofurane Type Antiarrhythmic Compound", Chirality
6, 329-336 (1994)
1993
- G. Albrecht, G. Ecker, I. Tumova: "Herstellung
und antiphlogistische Aktivität neuer 1-Benzoxepin-5-on-Derivate",
Sci.Pharm. 61, 161-168 (1993)
- L. Jirovetz, G. Ecker, W. Jäger, T. Heiss:
"Untersuchungen des Gehalts verschiedener Zwiebelchargen an
Blei, Cadmium, Quecksilber und Selen mittels Atomabsorpions-Spektroskopie",
Ernährung 17, 265 (1993)
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