-
Le Borgne, M., Marchand, P.,
Delovoye-Seiller, B., Robert, J.-M.,
Robert-Piessard, S., Le Baut G., Hartman
R.W., Palzer, M., New selective
nonsteroidal aromatase inhibitors: Synthesis and
inhibitory activity of 2,3 or 5-( a
-azolybenzyl)-1H-indoles, Bioorg. Med.
Chem. Lett. 1999, 9, 333-336.
-
Wachall, B.G., Hector, M.,
Zhuang, Y., Hartmann, R.W.,
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, Bioorg. Med. Chem. 1999,
7, 1913-1924.
-
Zhuang, Y., Hartmann,
R.W., Synthesis and evaluation of
azole-substituted 2-aryl-6-
methoxy-3,4-dihydronaphthalenes and
-naphthalenes as inhibitors of 17 a
-hydroxylase- C17,20-lyase (P450 17), Arch.
Pharm. Pharm. Med. Chem. 1999, 332,
25-30.
-
Baston, E., Hartmann,
R.W., N-substituted
4-(5-indolyl)benzoic acids. Synthesis and
evaluation of steroid 5 a -reductase type I and
II inhibitory activity, Bioorg. Med. Chem. Lett.
1999, 9, 1601-1606.
-
Hartmann, R.W.,
Frotscher, M.,
1-Imidazolylcarbonyloxy-substituted
tetrahydroquinolines and pyridines : Synthesis
and evaluation of P450 TxA2 inhibition, Arch.
Pharm. Pharm. Med. Chem. 1999, 332,
358-362.
-
Haider, N., Hartmann,
R.W., Steinwender, A., Synthesis of 2-
[ 2-(1-imidazolyl)ethyl ] -4-phenylcycloalka [
g ] phthalazin-1(2H)-ones as
thromboxane A 2 synthase inhibitors, Arch.
Pharm. Pharm. Med. Chem. 1999, 332,
408-409.
-
Zhuang, Y., Wachall, B.G.,
Hartmann, R.W., Novel imidazolyl and
triazolyl substituted biphenyl compounds:
Synthesis and evaluation as nonsteroidal
inhibitors of human 17 a -
hydroxylase-C17,20-lyase(P450 17), Bioorg. Med.
Chem., 2000, 8, 1245-1252
-
Jacobs, C., Frotscher, M.,
Dannhardt, G., Hartmann, R.W.,
1-Imidazolyl (alkyl) substituted di and
tetrahydroquinolines and analogs. Synthesis and
evaluation of dual inhibitors of P450 TxA 2 and
P450 arom, J. Med. Chem. 2000, 43,
1841-1851.
-
Picard, F., Baston, E.,
Reichert, W., Hartmann, R.W.,
Synthesis of N-substituted
piperidine-4-(benzylidene-4-carboxylic acids)
and evaluation as inhibitors of steroid-5 a
-reductase type 1 and 2, Bioorg. Med. Chem.,
2000, 8, 1479-1487.
-
Hartmann, R.W.,
Reichert, M., New nonsteroidal steroid 5 a
-reductase inhibitors. Syntheses and
structure-activity-studies on carboxamide
phenylalkyl-substituted pyridones and
piperidones, Arch. Pharm. Pharm. Med. Chem.,
2000, 333, 145-153.
-
Reichert, W., Jose, J.,
Hartmann, R.W., 5 a -reductase in
intact DU145 cells: Evidence for isozyme I and
evaluation of novel inhibitors, Arch. Pharm.
Pharm. Med. Chem., 2000, 333,
201-204.
-
Le Borgne, M., Duflos, M., Le
Baut, G., Nicholls, P.J., Hartmann R.W.,
Synthesis and biological evaluation of indole
derivatives acting as anti-inflammatory or
antitumoraldrugs, Ann. Pharm. Fr., 2000,
58,316-320.
-
Baston, E., Palusczak, A.,
Hartmann, R.W., 6-Substituted 1H-quinolin-2-ones
and 2-methoxy-quinolines: Synthesis and
evaluation as inhibitors of steroid 5 a
-reductases type 1 and 2, Eur. J. Med. Chem.,
2000, 35, 931-940.
-
Hartmann, R.W.,
Hector, M., Haidar, S., Ehmer, P., Jose, J.,
Synthesis and evaluation of novel steroidal
oximes as inhibitors of P450 17 (17 a
-hydroxylase / C17-20-lyase) and 5 a -reductase
1 and 2, J. Med. Chem., 2000, 43,
4266-4277.
-
Hartmann, R.W.,
Hector M., Wachall, B.G., Palusczak, A., Palzer,
M., Huch V., Veith, M., Synthesis and evaluation
of 17-aliphatic heterocycle substituted
steroidal inhibitors of 17 a -hydroxylase /
C17,20-lyase (P450 17), J. Med. Chem. 2000,
43, 4437-4445.
-
Kleber, A., Hartmann,
R.W., Jose. J., Development of an
improved in vitro model to study the adhesion of
tumor cells to the basement membrane, Pharm.
Pharmacol. Lett. 2000, 10,
55-58.
-
Ehmer, P.B., Jose, J.,
Hartmann, R.W., Development of a simple
and rapid assay for the evaluation of inhibitors
of human 17 a -hydroxylase-C 17,20-lyase
(P450c17) by coexpression of P450c17 with
NADPH-cytochrome-P450-reductase in
Escherichia coli, J. Steroid Biochem. Mol.
Biol., 2000, 75, 57-63.
-
Reichert, W.,
Hartmann, R.W., Jose, J., Stable
expression of the human 5 a -reductase -
isoenzymes type I and type II in HEK293 cells to
identify dual and selective inhibitors, J. Enz.
Inhib., 2001, 16, 47-53.
-
Recanatini, M., Bisi, A.,
Cavalli, A., Belluti, F., Gobbi, S., Rampa, A.,
Valenti, P., Palzer, M., Palusczak, A.,
Hartmann, R.W., A new class of non
steroidal aromatase inhibitors: Design and
synthesis of chromone and xanthone derivatives,
and inhibition of P450 enzymes aromatase and 17
a -hydroxylase/C17,20-lyase, J. Med. Chem.,
2001, 44, 672-680.
-
Reichert, W., Michel, A.,
Hartmann R.W., Jose, J., Stable
expression of human 5 a -re-ductase type II in
COS1 cells due to chromosomal gene integration:
a novel tool for inhibitor identification, J.
Steroid Biochem. Mol. Biol., 2001, 78,
275-284.
-
Kleber, A., Hartmann,
R.W., Jose, J., No effect of
thromboxane A 2 on the attachment of tumor cell
lines MDA MB 231, DU145, and U937 to the
basement membrane in an in-vitro model, J.
Cancer Res. Clin. Oncol., 2001, 127,
751-754.
-
Schertl, S.,
Hartmann, R.W., Batzl-Hartmann, C.,
Schlemmer, R., Spruß, T., Bernhardt, G., Gust,
R., Schönenberger, H.,
1-(2,6-Dichloro-4-hydroxyphenyl)-2-phenylethanes
- new biological response modifiers for the
therapy of breast cancer. Synthesis and
evalulation of estrogenic/antiestrogenic
properties, Arch. Pharm. Pharm. Med. Chem.,
2001, 334, 125-137.
-
Baston, E., Klein, C.D.P.,
Grimminger, W., Hebecker, N., Hartmann,
R.W., Synthesis, evaluation and QSAR
studies of highly potent aromatase inhibitors of
the piperidinedione type, Anti Cancer Drug Des.,
2001, 16, 37-47.
-
Haidar, S., Klein, C.D.P.,
Hartmann, R.W., Synthesis and
evaluation of steroidal hydro- xamic acids as
inhibitors of P450 17 (17 a
-hydroxylase/C17-20-lyase), Arch. Pharm. Pharm.
Med. Chem., 2001, 334, 138-140.
-
Hartmann, R. W.,
CYP-17-Inhibitoren: Steroidomimetika zur
Behandlung des Prostata- karzinoms, Pharm. Ztg.,
2001, 146, 2285-2289.
-
Hartmann, R.W.,
Die rationale Entwicklung eines Hemmstoffs von
CYP 17, einem neuartigen Target zur Behandlung
des Prostatacarcinoms, Magazin Forschung, UdS,
2001, 2, 2-9.
-
Lehr,C.-M., Hartmann,
R.W., Lenhof, H.-P., Das virtuelle
Biolabor, Pharm. Ztg., 2001, 146,
2541-2543.
-
Haidar, S., Ehmer, P.B.,
Hartmann, R.W., Novel Steroidal
Pyrimidyl Inhibitors of P450 17 (17
a-Hydroxylase/C17-20-Lyase), Arch. Pharm. Pharm.
Med. Chem., 2001, 334, 373-374.
-
Salem, O.I.A., Schulz, T.,
Hartmann, R.W., Synthesis and
biological evaluation of 4-(4- alkyl- and
Phenylaminocarbonyl)benzoyl)benzoic acid
derivatives as nonsteroidal inhibitors of
steroid 5 a -reductase isozymes 1 and 2, Arch.
Pharm. Pharm. Med. Chem., 2002, 335,
83-88.
-
Hartmann, R.W.,
Ehmer, P. B., Haidar, S., Hector, M., Jose, J.,
Klein, C.D.P., Seidel, S. B., Serge jew, T.,
Wachall, B. G., Wächter, G. A., and Zhuang Y.,
Review: inhibition of CYP 17, A new strategy for
the treatment of prostate cancer, Arch. Pharm.
Pharm. Med. Chem., 2002, 335,
119-128.
-
Picard, F., Schulz, T.,
Hartmann, R.W., 5-Phenyl substituted
1-methyl-2-pyridones and 4'-substituted
biphenyl-4-carboxylic acids. Synthesis and
evaluation as inhibitors of steroid-5 a
-reductase type 1 and 2, Bioorg. Med. Chem.,
2002, 10, 437-448.
-
Ehmer, P.B., Bureik, M.,
Bernhardt, R., Müller, U., Hartmann,
R..W., Development of a test system for
inhibitors of human aldosterone synthase
(CYP11B2): screening in fission yeast and
evaluation of selectivity in V79 cells, J.
Steroid Biochem. Mol. Biol., 2002, 81,
173-179.
-
Picard, F. and
Hartmann, R.W., N-substituted
4-(4-carboxyphenoxy)benzamides.Synthesis and
evaluation as inhibitors of steroid-5 a
-reductase type 1 and 2, J. Enzym. Inhib. Med.
Chem., 2002, 17, 187-196.
-
Picard, F., Barassin S.,
Mokhtarian, A., Hartmann, R.W.,
Synthesis and evaluation of 2’-substituted
4-(4’-carboxy- or
4’-carboxymethylbenzylidene)-N-acylpiperidines:
highly potent and In Vivo active
steroid 5 a -reductase type 2 inhibitors, J.
Med. Chem., 2002, 45,
3406-3417.
-
Haidar, S. and
Hartmann, R.W., C16 and C17 substituted
derivatives of pregnenolone and progesterone as
inhibitors of 17 a -hydroxylase-C17,20-lyase:
synthesis and biological evaluation, Arch.
Pharm. Pharm. Med. Chem., 2002, 335,
526-534.
-
Baston, E., Salem, O.I.A. and
Hartmann, R. W., 6-substituted
3,4-Dihydro-naphthalene-2-carboxylic acids:
synthesis and structure-activity studies in a
novel class of human 5 a reductase inhibitors,
J. Enz. Inhib. Med. Chem., 2002, 17,
303-320.
-
Mathur, S., Hassel, M.,
Steiner, F., Hollemayer, K., Hartmann,
R.W., Development of a new approach for
screening combinatorial libraries using
MALDI-TOF-MS and HPLC- ESI-MS/MS, J. Biomol.
Screening, 2003, 8, 136-148.
-
Hartmann, R.W.,
Müller, U., Ehmer, P.B., Discovery of selective
CYP11B2 (aldosterone synthase) inhibitors for
the therapy of congestive heart failure and
myocardial fibrosis, Eur. J. Med. Chem., 2003,
38, 363-366.
-
Baston, E. Salem, O.I.A.,
Hartmann, R.W., Cyclohex-1-ene
carboxylic acids: synthesis and biological
evaluation of novel inhibitors of human 5 a
reductase, Arch. Pharm. Pharm. Med. Chem., 2003,
336 , 31-38.
-
Haidar, S., Ehmer P.B.,
Barassin, S., Batzl-Hartmann, C.,
Hartmann, R.W., Effects of novel 17 a
-hydroxylase/C17, 20-lyase (P450 17, CYP 17)
inhibitors on androgen biosynthesis in vitro
and in vivo, J. Steroid. Biochem. Mol.
Biol., 2003, 84, 555-562.
-
Leroux, F., Hutschenreuter,
T., Charrière, C., Scopelliti, R.,
Hartmann, R.W., N
-(4-Biphenylmethyl)imidazoles as potential
therapeutics for the treatment of prostate
cancer: metabolic robustness due to fluorine
substition?, Helv. Chim. Act., 2003, 86,
2671-2686.
-
Marchand, P., Le Borgne, M.,
Palzer, M., Le Baut, G., Hartmann R.W.,
Preparation and pharmacological profile of 7-( a
-Azolylbenzyl)-1H-Indoles and indolines
as new aromatase inhibitors, Bioorg. Med. Chem.
Lett., 2003, 13, 1553-1555.
-
Aboul-Enein, H.Y., Hefnawy
M.M., Ehmer, P.B., Hartmann, R.W.,
Enantiomeric resolution of some human
aldosterone synthase [ CYP 11 B2 ] inhibitors on
derivatized polysaccharide chiral stationary
phases, J. Sep. Sci., 2003, 26,
1455-1458.
-
Clement, O.O., Freeman, C.M.,
Hartmann, R.W., Palusczak A.,
Handratta, V.D., Vasaitis, T.S., Brodie, A.M.H.,
Njar, V.C.O., Three Dimensional Pharmacophore
Modeling of Human CYP17 inhibitors: Potential
Agents for Prostate Cancer Therapy, J. Med.
Chem., 2003, 46, 2345-2351.
-
Hutschenreuter, T.U., Ehmer,
P.B., Hartmann, R.W., 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., 2004,
19, 17-32
-
Aboul-Enein, H.Y., Kladna,
A., Kruk, I., Lichszteld, K., Marchlewicz, M.,
Michalska, T., Salem, O.I.A., Hartmann,
R.W., Prooxidant and antioxidant action
of 4-(4-phenoxybenzoyl)benzoic acid derivatives,
Biopolymers, 2004, 73, 631-639.
-
Mathur, S., Picard, F.,
Dossou, U., Barassin, C., Seidel, S.B., Kang,
M.J., Hartmann, R.W.,
Evaluation of cell permeation of a potent
5α-reductase inhibitor using MALDI-TOF MS, J.
Enz. Inhib. Med. Chem., 2004, 19,
425-429
-
Hartmann, R.W.,
Palusczak, A., Lacan, F., Ricci, G., Ruzziconi,
R., CYP 17 and CYP 19 inhibitors. Evaluation of
fluorine effects on the inhibiting activity of
regioselectively fluorinated
1-(naphthalen-2-ylmethyl)imidazoles, J. Enz.
Inhib. Med. Chem., 2004, 19,
145-155.
-
Neugebauer, A., Klein,
C.D.P., Hartmann, R.W.,
Protein-dynamics of the putative HCV
receptorCD81 large extracellular loop, Bioorg.
Med. Chem.Lett., 2004, 14,
1765-1769.
-
Haider, S., Hartmann,
R.W., Inhibition of CYP 17, Potential
treatment of prostate cancer, Arab J. Pharm.
Sci., 2004, 2, 59-76
-
Gupta, R.B., Jindal, D.P.,
Jit, B., Narang, G., Palusczak, A.,
Hartmann, R.W., Synthesis and
evaluation of a dimer of
2-(4-pyridylmethyl)-1-indanone as a novel
nonsteroidal aromatase inhibitor, Arch. Pharm.
Pharm. Med. Chem., 2004, 337,
398-401.
-
Schertl, S.,
Hartmann, R.W., Batzl-Hartmann, C.,
Bernhardt, G., Spruß, T., Beckenlehner, K.,
Koch, M., Krauser, R., Schlemmer, R., Gust, R.,
Schönenberger, H.,
[1,2-Bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]platinum(II)
complexes, compounds for the endocrine therapy
of breast cancer – mode of action I: antitumor
activity due to the reduction of the endogenous
estrogen level, Arch. Pharm. Pharm. Med. Chem.,
2004, 337, 335-348.
-
Schertl, S.,
Hartmann, R.W., Batzl-Hartmann, C.,
Bernhardt, G., Spruß, T., Beckenlehner, K.,
Koch, M., Krauser, R., Schlemmer, R., Gust, R.,
Schönenberger, H.,
[1,2-Bis(2,6-difluoro-3-hydroxyphenyl)ethylenediamine]platinum(II)
complexes, compounds for the endocrine therapy
of breast cancer – mode of action II:
contribution of drug inactivation, cellular drug
uptake and sterical factors in the drug-target
interaction to the antitumor activity, Arch.
Pharm. Pharm. Med. Chem., 2004, 337,
349-359.
-
Kang, M.J., Mathur, S.,
Hartmann, R.W., Quantitative analysis
of 5α-reductase inhibitors in DU145 cells using
matrix-assisted laser desorption/ionisation
time-of-flight mass spectrometry and
high-performance liquid chromatography/tandem
mass spectrometry, J. Mass Spectrometry, 2004,
39, 762-769.
-
Hutter, M.C. and
Hartmann, R.W., QSAR of Human Steroid
5α-Reductase Inhibitors:
Where are the differences between isoenzyme type
1 and 2?, QSAR Comb. Sci ., 2004, 23,
406-415.
-
Lisurek, M., Kang, M.J.,
Hartmann, R.W., Bernhardt, R.,
Identification of monohydroxy progesterones
produced by CYP106A2 using comparative HPLC and
electrospray ionisation collision-induced
dissociation mass spectrometry, Biochem.
Biophys. Res. Comm., 2004, 319,
677-682.
-
Voets, M., Müller-Vieira, U.,
Marchais-Oberwinkler, S., Hartmann, R.W.,
Synthesis of amidinohydrazones and evaluation of
their inhibitory effect towards aldosterone
synthase (CYP11B2) and the formation of selected
steroids, Arch. Pharm. Pharm. Med. Chem., 2004,
337, 411-416.
-
Kang, M.J., Lisurek, M.,
Bernhardt, R., Hartmann R.W.,
Use of high-performance liquid
chromatography/electrospray ionization
collision-induced dissociation mass spectrometry
for structural identification of
monohydroxylated progesterones, Rapid Comm. in
Mass Spec., 2004, 18, 2795-2800
-
Leonetti, F., Favia, A., Rao,
A., Aliano, R., Paluszcak, A., Hartmann,
R.W., Carotti, A., Design, synthesis
and 3D QSAR of novel potent and selective
aromatase inhibitors, J. Med. Chem., 2004,
47, 6792-6803.
-
Lézé, M.P., Le Borgne, M.,
Marchand, P., Loquet, D., Kogler, M., Le Baut,
G., Palusczak, A., Hartmann, R.W.,
2- and 3-[(aryl)(azolyl)methyl]indoles as
potential non-steroidal aromatase inhibitors, J.
Enz. Inhib. Med. Chem., 2004, 19,
549-557.
-
Bild, T., Jose, J.,
Hartmann, R.W., Discovery of inhibitors
of the MCF-7 tumor cell adhesion to endothelial
cells and investigation on their mode of action,
Arch. Pharm. Pharm. Med. Chem., 2004,
337, 687-694.
-
Mathur, S., Park, J.D., Kim,
D.H., Hartmann, R.W., A Method
for Screening Enzyme Inhibitors Using Size
Exclusion Chromatography and ESI-LC-MS/MS, J.
Biomol. Screening, 2005, 10,
30-35.
-
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., Synthesis and
evaluation of
imidazolylmethylenetetrahydronaphthalenes and
imidazolylmethyleneindanes: potent inhibitors
of aldosterone synthase, J. Med. Chem., 2005, 48
, 1796-1805.
-
Haider, S., Hartmann,
R.W., Enzyme inhibitor examples for the
treatment of prostate tumor. In: Smith, H.J.,
Simons, C. (Hrsg.) Enzymes and their inhibition:
drug development, CRC Press, 2005, 241-253.
-
Streiber, M., Picard, F.,
Scherer, C., Seidel, S.B., Hartmann,
R.W., Methyl esters of N-(dicyclohexyl)acetyl-piperidine-4-(benzylidene-4-carboxylic
acids) as drugs and prodrugs: a new strategy for
dual inhibition of 5α-reductase type 1 and type
2, J. Pharm. Sci., 2005, 94,
473-480.
-
Ulmschneider,
S., Müller-Vieira, U., Klein, C.D.P., Antes, I.,
Lengauer, T.,
Hartmann, R.W.,
Synthesis and evaluation of
(pyridylmethylene)tetrahydronaphthalenes /
-indanes and structurally modified derivatives:
potent and selective inhibitors of
aldosterone synthase,
J. Med. Chem.
2005,
48,
1563-1575, Add. and Corr.
J. Med. Chem.
2005,
48,
4489-4490 .
-
Panter, B., Jose, J.,
Hartmann, R.W., 5 a -reductase in human
embryonic kidney cell line HEK293: evidence for
type II enzyme expression and activity, Mol.
Cell. Biochem., 2005, 270,
201-208.
-
Jindal, D.P., Bedi V., Jit,
B., Karkra, N., Guleria, S., Gupta, R.,
Palusczak, A., Hartmann, R.W.,
Synthesis and study of some new N-substituted
imide derivatives as potential anticancer
agents, Il Farmaco, 2005, 60,
283-290.
-
Angotti,
M., Hartmann R.W., Kirby, A.J.,
Simons, C., Nicholls, P.J., Sewell R.D.E.,
Smith, H.J., Effect of
2-(4-aminophenylmethyl)-6-hydroxy-3,4-dihydronaphthalen-1(2H)-one
on all-trans and 13-cis-retinoic acid levels in
plasma quantified by high performance liquid
chromatography coupled to tandem mass
spectrometry,
J. Enz.
Inhib. Med.
Chem.
2005,
20,
219-226.
-
Müller-Vieira, U., Angotti, M.,
Hartmann, R.W., The adrenocortical
tumor cell line NCI-H295R as an in vitro
screening system for the evaluation of
aldosterone synthase (CYP11B2) inhibitors and
their potential side effects,
J. Steroid Biochem.
Mol. Biol.
2005,
96,
259-270.
-
Voets,
M., Antes, I., Scherer, C., Müller-Vieira, U.,
Biemel, K., Barassin, C., Marchais-Oberwinkler,
S., Hartmann, R.W., Heteroaryl
substituted naphthalenes and structurally
modified derivatives: selective inhibitors of
CYP11B2 for the treatment of congestive heart
failure and myocardial fibrosis,
J. Med. Chem.,
2005,
48,
6632-6642.
-
Cavalli,
A., Bisi, A., Bertucci, C., Rosini, C.,
Paluszcak, A., Gobbi, S., Giorgio, E., Rampa,
A., Belluti, F., Piazzi, L., Valenti, P.,
Hartmann, R.W., Recanatini, M.,
Enantioselective
nonsteroidal aromatase inhibitors identified
through a multidisciplinary medicinal chemistry
approach,
J. Med.
Chem.,
2005,
48,
7282-7289.
-
Logé, C.,
Le Borgne, M., Marchand, P., Robert, J.-M.,
Palzer, M., Hartmann, R.W.,
Three-dimensional model of cytochrome P450 human
aromatase and docking studies in to the active
site,
J. Enz. Inhib. Med.
Chem.,
2005,
20,
581-585.
-
Ulmschneider, S., Negri, M., Voets, M.,
Hartmann, R.W., Development and
evaluation of a pharmacophore model for
inhibitors of aldosterone synthase (CYP11B2),
Bioorg. Med. Chem.
Lett.,
2006,
16,
25-30.
-
Lézé,
M.P., Le Borgne, M., Pinson, P., Palusczak, A.,
Duflos, M., Le Baut, G., Hartmann, R.W.,
Synthesis and biological evaluation of
5-[(aryl)(1H-imidazol-1-yl)methyl]-1H-indoles:
Potent and selective aromatase inhibitors,
Bioorg. Med. Chem.
Lett.,
2006,
16,
1134-1137.
-
Salem,
O.I.A., Frotscher, M., Scherer, C., Neugebauer,
A., Barassin, S., Streiber, M., Maas, R.,
Hartmann, R.W., Novel 5-Reductase
Inhibitors: Synthesis, Structure-Activity
Studies and Pharmacokinetic Profile of
Phenoxybenzoylphenyl Acetic Acids,
J. Med. Chem.,
2006,
49,
748-759.
-
Voets,
M., Antes, I., Scherer, C., Müller-Vieira, U.,
Biemel, K., Marchais-Oberwinkler, S.,
Hartmann, R.W., Synthesis and
Evaluation of Heteroaryl Substituted
Dihydronaphthalenes and Indenes: Potent and
Selective Inhibitors of Aldosterone Synthase
(CYP11B2) for the Treatment of Congestive Heart
Failure and Myocardial Fibrosis,
J. Med. Chem.,
2006,
49,
2222 -2231
-
Schuster,
D., Laggner, C., Steindl, T.M., Palusczak, A.,
Hartmann, R.W., Langer, T.;
Pharmacophore modeling and In Silico screening
for new P450 19 (Aromatase) Inhibitors,
J. Chem. Inf. Model.,
2006,
46,
1301-1311.
-
Görlitzer, K., Bonnekessel, Ch., Jones, P.G.,
Palusczak, A., Hartmann, R.W.,
Exemestan-Derivate – Synthese und Prüfung auf
Aromatase-Hemmung,
Die Pharmazie,
2006,
61,
575-582.
-
Gobbi,
S., Cavalli, A., Rampa, A., Belluti, F., Piazzi,
L., Paluszcak, A., Hartmann, R.W.,
Recanatini, M., Bisi, A., Lead optimization
providing a series of flavone derivatives as
potent nonsteroidal inhibitors of the cytochrome
P450 aromatase enzyme,
J. Med. Chem.,
2006,
49,
4777-4780
-
Jazbutyte,
V., Hu, K., Kruchten, P., Bey, E., Maier, S.,
Fritzemeier K.-H., Prelle, K., Hegele-Hartung,
C., Hartmann R.W., Neyses, L.,
Ertl, G., Pelzer, T., Ageing reduces the
efficacy of estrogen substitution to attenuate
cardiac hypertrophy in female SHR,
Hypertension,
2006,
48,
579-586
-
Engel, M., Hindie, V.,
Lopez-Garcia, L.A., Stroba, A., Schaeffer, F.,
Adrian, I., Imig, J., Idrissova, L.,
Nastainczyk, W., Zeuzem, S., Alzari, P.M.,
Hartmann, R.W., Piiper, A. and Biondi,
R.M., Allosteric activation of protein kinase
PDK1 with low molecular weight compounds,
EMBO J.,
2006,
23, 5469-5480
-
Drăgan,
C.A., Hartmann, R.W., Bureik,
M., A fission yeast based test system for the
determination of IC50 values of anti
prostate tumor drugs acting on CYP21,
J. Enz. Inhib. Med.
Chem.,
2006,
21,547-556
-
Schertl,
S., Hartmann, R.W.,
Batzl-Hartmann, C., Spruß, T., Maucher, A., von
Angerer, E., Schiller, C.D., Schneider, M.R.,
Gust, R., Schönenberger, H., Platinum(II)
complexes interfering with testicular steroid
biosynthesis: drugs for the therapy of advanced
or recurrent prostate cancers? Preclinical
studies,
Cancer Res Clin
Oncol,
2007,
133,
153-167
-
Hartmann, R.W.,
Müller-Vieira, U., Ulmschneider, S., Voets, M.,
Discovery of potent and selective inhibitors of
human aldosterone synthase (CYP11B2) – a new
target for the treatment of congestive heart
failure and myocardial fibrosis: A review, soon
to be submitted
-
Neugebauer, A. and
Hartmann, R.W., Protein-dynamics of
17β-hydroxysteroid dehydrogenase type 1
(17β-HSD1),
Bioorg. Med. Chem.
Lett., submitted
-
Scherer,
C., Dossou, U., Boettcher, S., Kang, M.J.,
Seidel, S.B., Hartmann, R.W., A
Novel Concept for BPH Therapy by Hybrid
Inhibition of 5α-Reductase Type 1 and Type 2:
Transport and Stability Studies in Caco-2 and
DU145 Cells,
Pharm. Res.,
submitted
-
Panter,
B., Jose, J., Hartmann, R.W.,
Protein characterisation of human steroid 5α-reductase
type II: Impact of posttranslational
modification on molecular weight and isoelectric
point,
Mol. Cell. Biochem.,
submitted
-
Boettcher, S., Werth, R.,
Hartmann, R.W., Immobilized
Enzymes for HTS of Chemical Libraries: Studies
Applying HPLC-ESI-MS/MS, soon to be submitted
-
Scherer,
C., Streiber, M., Dossou, U., Seidel, S.B.,
Boettcher, S., Kang, M.J.,
Hartmann, R.W., Evaluation of a
Novel Concept for BPH Therapy by Hybrid
Inhibition of 5α-Reductase
Type 1 and Type 2 using in Vitro Models, J.
Pharm. Sci., submitted
-
Neugebauer, A.,
Hartmann R. W., Klein, C.D.P.,
Identification of Protein-Protein-Interaction
Inhibitors by Chemoinformatics and Machine
Learning Methods, J. Med. Chem.,
submitted
-
Schertl, S., Hartmann,
R.W., Batzl-Hartmann, C., Spruß, T.,
Maucher, A., von Angerer, E., Schiller, C.D.,
Schneider, M.R., Gust, R., Schönenberger, H.,
Platinum(II) complexes interfering with
testicular steroid biosynthesis: drugs for the
therapy of advanced or recurrent prostate
cancers? Preclinical studies, Cancer Res
Clin Oncol, 2007, 133,
153-167
-
Gobbi, S., Cavalli, A., Negri,
M., Schewe K., Belluti F., Piazzi L.,
Hartmann, R. W.,
Recanatini M., Bisi A.,
Imidazolylmethylbenzophenones: a novel class of
potent and selective aromatase inhibitors,
J. Med. Chem., 2007, 50,
3420-3422
-
McCarthy, A., Hartmann
R. W., Abell, A., Evaluation of
4’-Substituted Bicyclic Pyridones as
non-steroidal Inhibitors of Steroid 5α-Reductase,
Bioorg. Med. Chem. Lett,
2007, 17, 3603-3607
-
Neugebauer, A.,
Hartmann, R. W., Klein, C.D.P.,
Prediciton of Protein-Protein Interaction
Inhibitors by Chemoinformatics and Machine
Learning Methods, J. Med. Chem.,
2007, 19,4665-4668
-
Le Borgne, M., Marchand, P.,
Nourrisson, M.R., Loquet, D., Palzer, M.,
Baston, E., Hartmann, R.W.,
Synthesis and biological evaluation of
3-(azolylmethyl)-1H-indoles and
3-(?-azolylbenzyl)-1H-indoles as selective
aromatase inhibitors, J. Enz.Inhib. and Med.
Chem., 2007, 22, 667-676
-
Pinto-Bazurco Mendieta, M.
A.E., Negri, M., Jagusch, C., Hille, U.E.,
Müller-Vieira, U., Schmidt, D., Hansen, K.,
Hartmann, R.W., Synthesis,
biological evaluation and molecular modeling
studies of novel ACD- and ABD-ring
steroidomimetics as inhibitors of CYP17,
Bioorg. Med. Chem.Lett. , 2008,
18, 267-273
-
Jagusch, C., Negri, M., Hille,
U.E., Hu, Q., Bartels, M., Jahn-Hoffmann, K.,
Pinto- Bazurco Mendieta M.A.E., Biemel, K.,
Rodenwaldt, B., Müller-Vieira, U., Schmidt, D.,
Lauterbach, T., Recanatinti, M., Cavalli, A.,
Hartmann, R.W., Synthesis,
biological evaluation and molecular modeling
studies of methyleneimidazole substituted
biaryls as inhibitors of human 17α
-hydroxylase- 17,20-lyase (CYP17) – Part
I:heterocyclic modifications of the core
structure, Bioorg. Med. Chem.,
2008, 16, 1992-2010
-
Frotscher, M., Ziegler, E.,
Marchais-Oberwinkler, S., Kruchten, P.,
Neugebauer, A., Fetzer, L., Scherer, C.,
Müller-Vieira, U., Messinger, J., Thole, H.,
Hartmann, R.W., Design,
Synthesis and Biological Evaluation of
(Hydroxyphenyl)- naphthalene and quinoline
derivatives: Potent, Selective and Non-Steroidal
Inhibitors of 17α
-Hydroxysteroid Dehydrogenase Type 1 (17α
-HSD1) for the Treatment of Estrogen-
Dependent Diseases,
J. Med. Chem., 2008,51,
2158-2169
-
Holzer, M., Ziegler, S.,
Kronenberger, B., Klein, C.D.P.,
Hartmann, R. W., Microwave assisted
syntheses of amino acid ester substituted
benzoic acid amides: Potential inhibitors of
human CD81-receptor HCV-E2 interaction, The
open Medicinal Chemistry Journal, 2008,
2, 21-25
-
Holzer, M., Ziegler, S.,
Albrecht, B., Kronenberger B., Bartenschlager
R., Kattner, L., Klein, C.D., Hartmann,
R. W., Identification of terfenadine as
an inhibitor of human CD81-receptor HCV-E2
interaction, synthesis and structure
optimization, Molecules, 2008,
13, 1081-1110
-
Hartmann, R.W.,
Müller-Vieira, U., Ulmschneider, S., Voets, M.,
Discovery of potent and selective inhibitors of
human aldosterone synthase (CYP11B2) – a new
target for the treatment of congestive heart
failure and myocardial fibrosis: A review, In:
Medicinal Chemistry: Chemical and Molecular
Aspects of Drug Design and Action, Taylor
and Francis/ CRC Publishing Company,
2008, 12,165- 175
-
Bey, E., Marchais-Oberwinkler,
Kruchten, P., S., Frotscher, M., Werth, R.,
Oster, A., Algul, Ö., Neugebauer, A.,,
Hartmann, R.W., Design, Synthesis and
Biological Evaluation of Bis(hydroxyphenyl)
azoles as Potent and Selective Non Steroidal
Inhibitors of 17ß-Hydroxysteroid Dehydrogenase
Type 1 (17ß-HSD1) for treatment of Estrogen
Dependant Diseases, Bioorg. Med Chem,
2008, 16,6423-6435
-
Holzer, M., Ziegler, S.,
Neugebauer, A., Kronenberger, B., Klein, C.D.P.,
Hartmann, R.W., Virtual
Screening and Structural Modification of
Salicylates: Inhibitors of Human CD81-Receptor
HCV-E2 Interaction, Arch. Pharm.Chem.Life
Sci., 2008, 341,478-484
-
Marchais-Oberwinkler, S. ,
Kruchten, P., Frotscher M., Ziegler, E.,
Neugebauer, Bhoga, U., Bey, E., Müller-Vieira,
U., Messinger, J., Thole, H., Hartmann,
R.W., Substituted 6-Phenyl-2-naphthols.
Potent and Selective Non-Steroidal Inhibitors of
17ß-Hydroxisteroid Dehydrogenase Type 1 (17
ß-HSD1): Design, Synthesis, Biological
Evaluation and Pharmacokinetics, J. Med.
Chem, 2008, doi
10.1021/jm800367 publ.on web 07/17/2008
-
Pinto-Bazurco Mendieta M.,
Negri, M., Hu, Q., Hille, U., Jagusch, C.,
Müller-Vieira, U., Jahn-Hoffmann, K., Schmidt,
D., Lauterbach, T., Hartmann, R.W.,
CYP17 inhibitors. Annulations of Additional
Rings in Methyleneimidazole Substituted
Biphenyls: Synthesis, Biological Evaluation and
Modelling, Arch. Pharm.Chem.Life Sci.,
in press
-
Hahner, S., Stürmer, A.,
Fassnacht, M., Hartmann, R.W.,
Schewe, K., Cochran S., Zink M., Schirbel A.,
Allolio B., Pleiotropic effects of etomidate in
adrenocortical cells – evidence for intraadrenal
regulation of steroidogenesis and profileration,
MCE, in press
-
Heim, R., Lucas, S. Grombein,
C., Voets, M., Negri, M., R.W. Hartmann,
Overcoming Undesirable CYP1A2 Potency of
Pyridylnaphthalene Type Aldosterone Synthase
Inhibitors: Influence of Heteroaryl Sustitution
on Potency and Selectivity ,J. Med. Chem,
in press
-
Pinto-Bazurco Mendieta M.,
Negri, M., Jagusch, C., Müller-Vieira, U.,
Lauterbach T., Hartmann, R. W.,
Synthesis, Biological Evaluation and Molecular
Modeling of Abiraterone Analogs: Novel CYP17
Inhibitors for the Treatment of Prostate Cancer,
J. Med. Chem, in press
-
Hu, Q., Negri, M.,
Jahn-Hoffmann, K., Zhuang,Y., Olgen, S.,
Bartels, M., Müller- Vieira, U., Schmidt, D.,
Lauterbach, T., Hartmann, R.W.,
Synthesis, Biological Evaluation and Molecular
Modelling Studies of Methylene Imidazole
Substituted Biaryls as Inhibitors of Human 17α
-hydroxylase-17, 20-lyase (CYP17) – Part
II: Core Rigidification and Influence of
Substituents at the Methylene Bridge,
Bioorg. Med Chem, in press
-
Pinto-Bazurco Mendieta M., Negri, M., Jagusch,
C., Müller-Vieira,
U., Lauterbach T.,
Hartmann, R. W.,
Synthesis, biological evaluation and molecular
modeling of
abiraterone analogs: Novel CYP17 inhibitors for
the treatment of prostate cancer,
J.
Med.Chem.,
2008,51,
5009-5018
-
Lucas, S., Heim, R., Negri, M., Antes, I., Ries,
C., Schewe, K., Bisi, A., Gobbi, S.,
Hartmann, R.W., Novel aldosterone
synthase inhibitors with extended carbocyclic
skeleton by a combined ligand-based and
structure-based drug design approach,
J.
Med.Chem.
,2008,
51,
6138-6149
-
Castellano, S., Stefancich, G., Ragno, R.,
Schewe, K., Santoriello M., Caroli, A.,
Hartmann, R.W.,
Sbardella, G., CYP19 (Aromatase): Exploring the
scaffold flexibility for novel selective inhibitors, Bioorg. Med.Chem.,
2008,
18, 8349-8358.
-
Pinto-Bazurco Mendieta M., Negri, M., Hu, Q.,
Hille, U., Jagusch, C., Müller-Vieira, U.,
Jahn-Hoffmann, K., Schmidt, D., Lauterbach, T.,
Hartmann, R.W., CYP17
inhibitors. Annulations of additional rings in
methyleneimidazole substituted biphenyls:
Synthesis, biological evaluation and modelling,
Arch. Pharm.Chem.Life Sci.,
2008, 341, 597-609
-
Léze, M.-P., Palusczak, A., Hartmann,
R.W., Le Borge M., Synthesis of 6- or
4-functionalized indoles via a reductive
cyclization approach and evaluation as aromatase
inhibitors, Bioorg. Med.Chem.,
2008, 18, 4713- 47
-
Bey, E., Marchais-Oberwinkler, S., Werth, R.,
Negri, M., Al-Soud, Y., Kruchten, P., Oster A.,
Frotscher, M., Birk, B., Hartmann, R.W.,
Design, synthesis, biological evaluation and
pharmacokinetics of bis(hydroxyphenyl)substituted
azoles, thiophenes, benzenes and aza-benzenes as
potent and selective non-steroidal inhibitors of
17 ß - hydroxysteroid dehydrogenase type 1
(17ß-HSD1), J.Med.Chem., 2008,
51, 6725-6739
-
Gaube, F., Wölfl, S., Pusch, L., Werner, U.,
Kroll, T.C., Schrenk, D., Hartmann R.W.,
Hamburger M., Effects of Leuzea carthamoides DC.
On human breast adenocarcinoma MCF-7 cells
determined by gene expression profiling and
functional assays, Planta Medica,
2008, 74,1701-1708
-
Lucas, S., Heim, Ries, C., Schewe, K., Birk B.,
Hartmann R.W., 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., 2008,
51,8077-8087
-
Marchais-Oberwinkler, S., Frotscher, M.,
Ziegler, E., Werth, R., Kruchten, P., Messinger,
J., Thole, H., Hartmann, R.W.,
Structure-activity study in the class of 6-(3’-hydroxyphenyl)
naphthalenes leading to an optimization of a
pharmacophore model for 17beta-hydroxysteroid
dehydrogenase type1 (17beta-HSD1) inhibitors,
Mol.Cell.Endocrino., 2009,
301,205-211
-
Marchais-Oberwinkler, S., Frotscher, M.,
Ziegler, E., Werth, R., Kruchten, P., Messinger,
J., Thole, H., Hartmann, R.W.,
Structure-activity study in the class of 6- (3’-hydroxyphenyl)naphthalenes
leading to an optimization of a pharmacophore
model for 17beta-hydroxysteroid dehydrogenase
type1 (17beta-HSD1) inhibitors, Mol. Cell.
Endocrinol. 2009, 301, 205-211
-
Kruchten, P., Werth, R., Marchais-Oberwinkler,
S., Frotscher, M., Hartmann, R.W.,
Development of a biological screening system
fort the evaluation of highly active and
selective 17beta-HSD1-inhibitors as potential
therapeutic agens, Mol. Cell. Endocrinol.
2009, 301, 154-157
-
Al-Soud, Y. A., Bey, E., Oster A.,
Marchais-Oberwinkler, S.,Werth, R., Kruchten,
P., Frotscher, M., Hartmann, R.W.,
The role of the heterocycle in bis(hydroxyphenyl)triazoles
for inhibition of 17beta-hydroxysteroid
dehydrogenase (17beta- HSD) type 1 and type 2,
Mol. Cell. Endocrinol. 2009,
301, 212-215
-
Kruchten, P., Werth, R., Bey, E., Oster, A.,
Marchais-Oberwinkler, S., Frotscher, M.,
Hartmann, R.W., Selective inhibition of
17beta-hydroxysteroid dehydrogenase type 1
(17betaHSD1) reduces estrogen responsive cell
growth of T47-D breast cancer cells, J. Steroid
Biochem. Mol. Biol. 2009, 114,
200-206
-
Hille, U., Hu Q., Bartels, M., Müller-Vieira,
U., Schmidt, D., Lauterbach, T., Hartmann, R.W.,
Novel CYP17 inhibitors: Synthesis, biological
evaluation, structure- activity relationships
and modelling of methoxy-and hydroxy-substituted
methyleneimidazolyl biphenyls, Eur. J. Med.
Chem. 2009, 44, 2765-2775
-
Ries, C., Lucas, S., Heim, R., Birk, B.,
Hartmann, R.W., Selective aldosterone
synthase inhibitors reduce aldosterone formation
in vitro and in vivo, J. Steroid Biochem. Mol.
Biol. 2009, 116, 121-126
-
Stroba, A., Schaeffer, F., Hindie, V.,
Lopez-Garcia, L., Adrian, I., Fröhner, W.,
Hartmann, R.W., Biondi, R.M.,
Engel, M., 3,5-Diphenylpent-2-enoic acids as
allosteric activators of the protein kinase
PDK1: Structure-activity relationships and
thermodynamic characterisation of binding as
paradigms for PIF-binding pocket- targeting
compounds, J. Med. Chem. 2009,
15, 4683-4693.
-
Ziegler, S., Kronenberger B., Albrecht B. A.-M.,
Kaul A., Gamer A.-L., Klein, C.D.,
Hartmann, R.W., Development and
evaluation of a FACS-based medium throughput
assay for HCV entry inhibitors, J. Biomol.
Screening 2009, 6, 620-626
-
Kruchten, P., Werth, R., Marchais-Oberwinkler,
S., Bey, E., Ziegler E., Oster A. Frotscher, M.,
Hartmann, R.W., Development of
biological assays for the identification of
selective inhibitors of estradiol formation from
estrone in rat liver preparations, Comptes
Rendus Chimie 2009, 12,
1110-1116
-
Hille, U., Hu, Q., Pinto-Bazurco Mendieta, M.,
Bartels, M., Vock, C.A., Lauterbach, T.,
Hartmann, R.W., Steroidogenic
cytochrome P450 (CYP) enzymes as drug targets:
Combining substructures of known CYP inhibitors
leads to compounds with different inhibitory
profile, Comptes Rendus Chimie 2009,
12, 1117-1126
-
Bey, E., Marchais-Oberwinkler, S., Negri, M.,
Kruchten, P., Oster A., Klein, T., Spadaro. A.,
Werth, R., Frotscher, M., Birk, B.,
Hartmann, R.W., New insights into the
SAR and binding modes of bis(hydroxyphenyl)thiophenes
and benzenes: Influence of additional
substituents on 17 ß-hydroxysteroid
dehydrogenase type 1 (17ß-HSD1) inhibitory
activity and selectivity, J. Med. Chem.
2009, 52, 6724-6743
-
Hu, Q., Negri, M., Olgen, S., Hartmann,
R.W., The role of fluorine Substitution
in biphenyl methylene imidazole type CYP17
inhibitors for the treatment of prostate
carcinoma, ChemMedChem 2010, 5,
899-910
-
Oster, A., Klein, T., Werth, R., Kruchten, P.,
Bey, E., Negri, M., Marchais- Oberwinkler, S.,
Frotscher, M., Hartmann, R.W.,
Novel estrone mimetics with high 17β-HSD1
inhibitory activity, Bioorg. Med. Chem.
2010, 18, 3494-3505
-
Haller, F., Moman, E., Hartmann, R.W.,
Adamski, J., Mindnich, R., Molecular framework
of steroid/retinoid discrimination in
17beta-hydroxysteroid dehydrogenase type 1 and
photoreceptor-associated retinol dehydrogenase,
J. Mol. Biol. 2010, 399,
255-267
-
Bansal, R. Guleria, S., Ries, C.,
Hartmann R.W., Synthesis and
antineoplastic activity of O-alkylated
derivatives of 7-hydroximinoandrost-5-ene
steroids, Arch. Pharm. Chem. Life Sci.
2010, 343, 377-383
-
Negri, M., Recanatini, M., Hartmann,
R.W., Insights in 17β-HSD1 enzyme
kinetics and ligand binding by fynamic motion
investigation, PloS One 2010,
5, e12026
-
Welker, M.-W., Von Wagner, M., Ochs, D. Zimmer,
V., Hofmann, W.P., Piiper, A., Hartmann,
R.W., Herrmann, E., Zeuzem, S.,
Kronenberger, B., Influence of amantadine on
CD81 expression on lymphocytes in chronic
hepatitis C, Digestive and Liver Disease
2010, 42, 735-740
-
Hu, Q., Jagusch, C., Hille, U., Haupenthal, J.,
Hartmann, R.W., Replacement of
imidazolyl by pyridyl in biphenylmethylenes
results in selective CYP17 and dual
CYP17/CYP11B1 inhibitors for the treatment of
prostate cancer, J. Med. Chem. 2010,
53, 5749-5758
-
Gobbi, S., Zimmer, C., Belluti, F., Rampa, A.,
Hartmann, R.W., Recanatini, M.,
Bisi, A., Novel highly potent and selective
nonsteroidal aromatase inhibitors: Synthesis,
biological evaluation and strucure -activity
relationships investigation, J. Med. Chem.
2010, 53, 5347-5351
-
Hu, Q., Yin, L., Jagusch, C., Hille, U.E.,
Hartmann, R.W., Isopropylidene
substitution increases activity and selectivity
of biphenylmethylene 4-pyridine type CYP17
inhibitors, J. Med. Chem. 2010,
53, 5049-5053
-
Hahner, S., Stürmer, A., Fassnacht, M.,
Hartmann, R.W., Schewe, K., Cochran S.,
Zink M., Schirbel A., Allolio B., Etomidate
unmasks intraadrenal regulation of
steroidogensis and proliferation in adrenal
cortical cell lines, Horm. Metab. Res.
2010, 42, 528-534
-
Reum, N., Fink-Straube, C., Klein, T.,
Hartmann, R.W., Lehr, C.-M., Schneider,
M., Multilayer coating of gold nanoparticles
with drug-polymer coadsorbates, Langmuir
2010, 26, 16901-16908
-
Oster, A., Hinsberger, S., Werth R., Marchaise-Oberwinkler,
S., Frotscher, M., Hartmann, R.W.,
Bicyclic substituted hydroxyphenylmethanones as
novel inhibitors 17β-HSD1 for the treatment of
estrogen-dependent diseases, J. Med. Chem. 2010,
53, 8176-8186
-
Heinzerling, L., Hartmann, R.W.,
Frotscher, M., Neumann, D., Predicting putative
inhibiors of 17β-HSD1, Mol. Inf. 2010,
29, 695-705
-
Zimmer, C., Hafner, M., Zender, M., Amman, D.,
Hartmann, R.W., Vock, C.A., N-
(pyridin-3-yl)benzamides as selective inhibitors
of human aldosterone synthase (CYP11B2), Bioorg.
Med. Chem. Lett. 2011, 21,
186-190
-
Wetzel, M., Marchais-Oberwinkler, S.
Hartmann, R.W., 17-HSD2 inhibitors for
the treatment of osteoporosis: Identification of
a promising scaffold, Bioorg. Med. Chem. 2011,
19, 807-815
-
Mohamed, A. H., Ba-Bernardi, L., Burkholz T.,
Schumann, E., Diesel, B., Zapp, J., Kiemer,
A.K., Ries, C., Hartmann, R.W.,
Hosny M., Jacob, C., Facile synthesis of chrysin-derivatives
with promising activities as aromatase
inhibitors, NPC 2011, 6, 31-34
-
Marchais-Oberwinkler, S., Wetzel, M., Ziegler,
E., Kruchten, P., Werth, R., Henn, C.,
Hartmann, R.W., New drug-like
hydroxyphenylnaphthol steroidomimetics as potent
and selective 17b-HSD1 inhibitors for the
treatment of estrogen-dependent diseases, J.
Med. Chem. 2011, 54, 534-547
-
Hille, U. E., Zimmer, C., Vock, C.A.,
Hartmann, R.W., First selective CYP11B1
inhibitors for the treatment of cortisol
dependent diseases, Med. Chem. Lett.
2011, 2, 2-6
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