Helmholtz-Zentrum für Infektionsforschung

Helmholtz-Zentrum für Infektionsforschung

Vollständige Publikationsliste der Abteilung DDOP (Rolf W. Hartmann)

 

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Ausgewählte Publikationen

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Negri,M.; Recanatini,M.; Hartmann,Rolf W.*; (2011). Computational investigation of the binding mode of bis(hydroxylphenyl)arenes in 17beta-HSD1: molecular dynamics simulations, MM-PBSA free energy calculations, and molecular electrostatic potential maps1. Journal of Computer-Aided Molecular Design: 25 9, 795-811

Hille UE, Zimmer C, Vock CA, Hartmann RW; (2011). First selective steroid-11β-hydroxylase (CYP11B1) inhibitors for the treatment of cortisol dependent diseases. Med Chem Lett.: 2 1, 2-6

Marchais-Oberwinkler S, Henn C, Möller G, Klein T, Negri M, Oster A, Spadaro A, Werth R, Wetzel M, Xu K, Frotscher M, Hartmann RW, Adamski J; (2010). 17β-Hydroxysteroid dehydrogenase (17β-HSDs): Genes, protein structures, novel therapeutic targets and recent progress in inhibitor development. J Steroid Biochem Mol Biol.: 125, 66-82

Oster A, Hinsberger S, Werth R, Marchais-Oberwinkler S, Frotscher M, Hartmann RW; (2010). Bicyclic substituted hydroxyphenylmethanones as novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases. J Med Chem.: 53 22, 8176-8186 PubMed

Negri,M.; Recanatini,M.; Hartmann,R.W.*; (2010). Insights in 17beta-HSD1 enzyme kinetics and ligand binding by dynamic motion investigation. PLoS ONE: 5 8, e12026

Reum N, Fink-Straube C, Klein T, Hartmann RW, Lehr CM, Schneider M; (2010). Multilayer coating of gold nanoparticles with drug-polymer coadsorbates. Langmuir.: 26 22, 16901-16908 PubMed

Marchais-Oberwinkler S, Wetzel M, Ziegler E, Kruchten P, Werth R, Henn C, Hartmann RW; (2010). New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-HSD1 inhibitors for the treatment of estrogen-dependent diseases. J Med Chem.: 54 2, 534-547 PubMed

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 15, 5749-5758

Ziegler S, Kronenberger B, Albrecht BA, Kaul A, Gamer AL, Klein CD, Hartmann RW; (2009). Development and evaluation of a FACS-based medium throughput assay for HCV entry inhibitors. J Biomol Screen.: 14 6, 620-626 PubMed

Bey E, Marchais-Oberwinkler S, Negri M, Kruchten P, Oster A, Klein T, Spadaro A, Werth R, Frotscher M, Birk B, Hartmann RW; (2009). New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17ß-hydroxysteroid dehydrogenase type 1 (17ß-HSD1) inhibitory activity and selectivity. J Med Chem.: 52 21, 6724-6743 PubMed

Bey E, Marchais-Oberwinkler S, Werth R, Negri M, Al-Soud YA, Kruchten P, Oster A, Frotscher M, Birk B, Hartmann RW; (2008). Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl)substituted azoles, thiophenes, benzenes and aza-benzenes as potent and selective non-steroidal inhibitors of 17ß-hydroxysteroid dehydrogenase type 1 (17ß-HSD1). J Med Chem.: 51 21, 6725-6739 PubMed

Lucas S, Heim R, Ries C, Schewe KE, Birk B, Hartmann RW; (2008). In vivo active aldosterone synthase inhibitors with improved selectivity: Lead optimization providing a series of pyridine substituted 3,4-dihydro-1H-quinolin-2-one derivates. J Med Chem.: 51 24, 8077-8087 PubMed

Heim R, Lucas S, Grombein CM, Ries C, Schewe KE, Negri M, Müller-Vieira U, Birk B, Hartmann RW; (2008). Overcoming undesirable CYP1A2 potency of pyridylnaphthalene type aldosterone synthase inhibitors: Influence of heteroaryl substitution on potency and selectivity. J Med Chem.: 51 16, 5064-5074 PubMed

Pinto-Bazurco Mendieta MA, Negri M, Jagusch C, Hille UE, Müller-Vieira U, Schmidt D, Hansen K, Hartmann RW; (2008). Synthesis, biological evaluation and molecular modeling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17. Bioorg Med Chem Lett.: 18 1, 267-273 PubMed

Salem, O.I.A., Frotscher, M., Scherer, C., Neugebauer, Biemel, K., S., Streiber, M., Maas, R., Hartmann, R.W.; (2006). Novel 5α-reductase inhibitors: Synthesis, structure-activity studies and pharmacokinetic profile of phenoxybenzoylphenyl acetic acids. J. Med. Chem.: 49, 748-759 PubMed

Voets, M., Antes, I., Scherer, C., Müller-Vieira, U., Biemel, K., Barassin, C., Marchais-Oberwinkler, S., Hartmann, R.W.; (2005). Heteroaryl substituted naphthalenes and structurally modified derivatives: selective inhibitors of CYP11B2 for the treatment of congestive heart failure and myocardial fibrosis. J. Med. Chem.: 48, 6632-6642 PubMed

Ulmschneider, S., Müller-Vieira, U., Mitrenga, M., Hartmann, R.W., Marchais-Oberwinkler, S., Klein, C.D.P., Bureik, M., Bernhardt, R., Antes, I., Lengauer, T.; (2005). Synthesis and evaluation of imidazolylmethylenetetrahydronaphthalenes and imida-zolylmethyleneindanes: potent inhibitors of aldosterone synthase. J. Med. Chem.: 48, 1796-1805 PubMed

Hutschenreuter, T.U., Ehmer, P.B., Hartmann, R.W.; (2004). Synthesis of hydroxy derivatives of highly potent non-steroidal CYP 17 inhibitors as potential metabolites and evaluation of their activity by a non cellular assay using recombinant human enzyme. J. Enz. Inhib. Med. Chem.: 19, 17-32 PubMed

Ehmer, P.B., Bureik, M., Bernhardt, R., Müller, U., Hartmann, R..W.; (2002). Development of a test system for inhibitors of human aldosterone synthase (CYP11B2): screening in fission yeast and evaluation of selectivity in V79 cells. J. Steriod Biochem. Mol. Biol.: 81, 173-179 PubMed

Ehmer, P.B., Jose, J., Hartmann, R.W.; (2000). Development of a simple and rapid assay for the evaluation of inhibitors of human 17α-hydroxylase-C17,20-lyase (P450c17) by coexpression of P450c17 with NADPH-cytochrome-P450-reductase in Escherichia coli. J. Steroid Biochem. Mol. Biol.: 75, 57-63 PubMed

Hartmann, R.W., Hector, M., Haidar, S., Ehmer, P., Jose, J.; (2000). Synthesis and evaluation of novel steroidal oximes as inhibitors of P450 17 (17α-hydroxylase / C17-20-lyase) and 5α-reductase 1 and 2. J. Med. Chem.: 43, 4266-4277 PubMed

Wachall, B.G., Hector, M., Zhuang, Y., Hartmann, R.W.; (1999). Imidazole substituted biphenyls - a new class of highly potent and in vivo active inhibitors of P450 17 as potential therapeutics for treatment of prostate cancer. Bioog. Med. Chem.: 7, 1913-1924 PubMed

Wächter, G.A., Hartmann, R.W., Sergejew, T., Grün, G.L., Ledergerber, D. ; (1996). Tetrahydronaphthalenes: Influence of heterocyclic substituents on inhibition of steroidogenic enzymes P450 arom and P450 17. J. Med. Chem.: 39, 834-841 PubMed

Hartmann, R.W., Bayer, H., Grün, G.; (1994). Aromatase inhibitors. Syntheses and structure-activity studies of novel pyridyl-substituted indanones, indans and tetralins. J. Med. Chem.: 37, 1275-1281 PubMed

Sergejew, T., Hartmann, R.W.; (1994). Pyridyl substituted benzocycloalkenes: New inhibitors of 17α-hydroxylase / 17,20-lyase (P450 17α)). J. Enz. Inhib.: 8, 113-122 PubMed

Hartmann, R.W., Batzl, C.; (1986). Aromatase inhibitors. Synthesis and evaluation of mammary tumor inhibiting activity of 3-alkylated 3-(4-aminophenyl)piperidine-2,6-diones. J. Med. Chem.: 29, 1362-1369 PubMed

Hartmann, R.W., Kranzfelder, G., v. Angerer, E., Schönenberger, H.; (1980). Antiestrogens. Synthesis and evaluation of mammary tumor inhibiting activity of 1,1,2,2-tetraalkyl-1,2-diphenylethanes. J. Med. Chem.: 23, 841-848 PubMed

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21.05.2012