Ergebnisbericht 2010/11 - Helmholtz-Zentrum für Infektionsforschung

• Khvedelidze,M., Mdzinarashvili,T., Partskhaladze,T., Nafee,N.,
Schaefer,U.F., Lehr,C.-M., & Schneider,M. (2011) Calorimetric and
spectrophotometric investigation of PLGA nanoparticles and their
complex with DNA. Journal of Thermal Analysis and Calorimetry 99,
337-348.
• Maurer,F., Daum,N., Schaefer,U.F., Lehr,C.-M., & Bauer,P. (2011) Plant
genetic factors for iron homeostasis affect iron bioavailability in
Caco-2 cells. Food Research International 43, 1661-1665.
• Patzelt,A., Richter,H., Knorr,F., Schafer,U., Lehr,C.-M., Dahne,L.,
Sterry,W., & Lademann,J. (2011) Selective follicular targeting by
modifi cation of the particle sizes. Journal of Control Release 150,
45-48.
• Schulze,C., Schaefer,U.F., Ruge,C.A., Wohlleben,W., & Lehr,C.-M.
(2011) Interaction of metal oxide nanoparticles with lung surfactant
protein A. European Journal of Pharmaceutics and Biopharmaceutics
77, 376-383.
Abt. für Wirkstoff-Design und -Optimierung – HIPS |
Prof. Dr. Rolf Hartmann
• Gobbi,S., Zimmer,C.*., Belluti,F., Rampa,A., Hartmann,R.W.*.,
Recanatini,M., & Bisi,A. (2010) Novel highly potent and selective
nonsteroidal aromatase inhibitors: synthesis, biological evaluation
and structure-activity relationships investigation. Journal of
Medicinal Chemistry 53, 5347-5351.
• Haller,F., Moman,E., Hartmann,R.W.*., Adamski,J., & Mindnich,R.
(2010) Molecular framework of steroid/retinoid discrimination in
17beta-hydroxysteroid dehydrogenase type 1 and photoreceptorassociated
retinol dehydrogenase. Journal of Molecular Biology 399,
255-267.
• Hu,Q., Yin,L., Jagusch,C., Hille,U.E., & Hartmann,R.W.*. (2010) Isopropylidene
substitution increases activity and selectivity of biphenylmethylene
4-pyridine type CYP17 inhibitors. Journal of Medicinal
Chemistry 53, 5049-5053.
• Hu,Q., Jagusch,C., Hille,U.E., Haupenthal,J., & Hartmann,R.W.*.
(2010) Replacement of imidazolyl by pyridyl in biphenylmethylenes
results in selective CYP17 and dual CYP17/CYP11B1 inhibitors for
the treatment of prostate cancer. Journal of Medicinal Chemistry 53,
5749-5758.
• Hu,Q., Negri,M., Olgen,S., & Hartmann,R.W. (2010) The role of
fl uorine substitution in biphenyl methylene imidazole-type CYP17
inhibitors for the treatment of prostate carcinoma. ChemMedChem 5,
899-910.
• Negri,M., Recanatini,M., & Hartmann,R.W.*. (2010) Insights in
17beta-HSD1 enzyme kinetics and ligand binding by dynamic
motion investigation. PLoS ONE 5, e12026.
• Oster,A., Hinsberger,S., Werth,R., Marchais-Oberwinkler,S.,
Frotscher,M., & Hartmann,R.W.*. (2010) Bicyclic substituted hydroxyphenylmethanones
as novel inhibitors of 17beta-hydroxysteroid
dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogendependent
diseases. Journal of Medicinal Chemistry 53, 8176-8186.
• Oster,A., Klein,T., Werth,R., Kruchten,P., Bey,E., Negri,M., Marchais-
Oberwinkler,S., Frotscher,M., & Hartmann,R.W.*. (2010) Novel
estrone mimetics with high 17beta-HSD1 inhibitory activity. Bioorganic
and Medicinal Chemistry 18, 3494-3505.
• Reum,N., Fink-Straube,C., Klein,T., Hartmann,R.W.*., Lehr,C.-M., &
Schneider,M. (2010) Multilayer coating of gold nanoparticles with
drug-polymer coadsorbates. Langmuir 26, 16901-16908.
• Zimmer,C., Hafner,M., Zender,M., Ammann,D., Hartmann,R.W.*., &
Vock,C.A. (2010) N-(Pyridin-3-yl)benzamides as selective inhibitors
of human aldosterone synthase (CYP11B2). Bioorganic and Medicinal
Chemistry Letters 21, 186-190.
WISSENSCHAFTLICHER ERGEBNISBERICHT | Veröffentlichungen
169
• Heinzerling,L., Hartmann,R.W.*., Frotscher,M., & Neumann,D. (2011)
Predicting putative inhibitors of 17beta-HSD1. Molecular Informatics
29, 695-705.
• Hille,U.E., Zimmer,C., Vock,C.A., & Hartmann,R.W.*. (2011) First
selective CYP11B1 inhibitors for the treatment of cortisol-dependent
diseases. ACS Medicinal Chemistry Letters 2, 2-6.
• Marchais-Oberwinkler,S., Wetzel,M., Ziegler,E., Kruchten,P.,
Werth,R., Henn,C., Hartmann,R.W.*., & Frotscher,M. (2011) New
drug-like hydroxyphenylnaphthol steroidomimetics as potent and
selective 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for
the treatment of estrogen-dependent diseases. Journal of Medicinal
Chemistry 54, 534-547.
• Oster,A., Klein,T., Henn,C., Werth,R., Marchais-Oberwinkler,S.,
Frotscher,M., & Hartmann,R.W.*. (2011) Bicyclic substituted hydroxyphenylmethanone
type inhibitors of 17 beta-hydroxysteroid dehydrogenase
Type 1 (17 beta-HSD1): the role of the bicyclic moiety.
ChemMedChem 6, 476-487.
• Stefanachi,A., Favia,A.D., Nicolotti,O., Leonetti,F., Pisani,L., Catto,M.,
Zimmer,C., Hartmann,R.W.*., & Carotti,A. (2011) Design, Synthesis,
and Biological Evaluation of Imidazolyl Derivatives of 4,7-Disubstituted
Coumarins as Aromatase Inhibitors Selective over 17-alpha-
Hydroxylase/C17-20 Lyase. Journal of Medicinal Chemistry 54, 1613-
1625.
• Wetzel,M., Marchais-Oberwinkler,S., & Hartmann,R.W.*. (2011)
17beta-HSD2 inhibitors for the treatment of osteoporosis: Identifi cation
of a promising scaffold. Bioorganic and Medicinal Chemistry 19,
807-815.
• Yadav,M.R., Sabale,P.M., Giridhar,R., Zimmer,C., Haupenthal,J., &
Hartmann,R.W.*. (2011) Synthesis of some novel androstanes as
potential aromatase inhibitors. Steroids 76, 464-470.