Search Results - "Bey, Emmanuel"

Hydroxybenzothiazoles as new nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) by Spadaro, Alessandro, Negri, Matthias, Marchais-Oberwinkler, Sandrine, Bey, Emmanuel, Frotscher, Martin

“…17β-estradiol (E2), the most potent estrogen in humans, known to be involved in the development and progession of estrogen-dependent diseases (EDD) like breast…”
Get full text

New Insights into the SAR and Binding Modes of Bis(hydroxyphenyl)thiophenes and -benzenes: Influence of Additional Substituents on 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) Inhibitory Activity and Selectivity by Bey, Emmanuel, Marchais-Oberwinkler, Sandrine, Negri, Matthias, Kruchten, Patricia, Oster, Alexander, Klein, Tobias, Spadaro, Alessandro, Werth, Ruth, Frotscher, Martin, Birk, Barbara, Hartmann, Rolf W

“…17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is responsible for the catalytic reduction of weakly active E1 to highly potent E2. E2 stimulates the…”
Get full text

Design, Synthesis, Biological Evaluation and Pharmacokinetics of Bis(hydroxyphenyl) substituted Azoles, Thiophenes, Benzenes, and Aza-Benzenes as Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) by Bey, Emmanuel, Marchais-Oberwinkler, Sandrine, Werth, Ruth, Negri, Matthias, Al-Soud, Yaseen A, Kruchten, Patricia, Oster, Alexander, Frotscher, Martin, Birk, Barbara, Hartmann, Rolf W

“…17β-Estradiol (E2), the most potent female sex hormone, stimulates the growth of mammary tumors and endometriosis via activation of the estrogen receptor α…”
Get full text

Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study by Abdelsamie, Ahmed S., van Koppen, Chris J., Bey, Emmanuel, Salah, Mohamed, Börger, Carsten, Siebenbürger, Lorenz, Laschke, Matthias W., Menger, Michael D., Frotscher, Martin

“…Current endocrine therapeutics for the estrogen-dependent disease endometriosis often lead to considerable side-effects as they act by reducing estrogen action…”
Get full text

Towards the evaluation in an animal disease model: Fluorinated 17β-HSD1 inhibitors showing strong activity towards both the human and the rat enzyme by Abdelsamie, Ahmed S., Bey, Emmanuel, Gargano, Emanuele M., van Koppen, Chris J., Empting, Martin, Frotscher, Martin

“…17β-Estradiol (E2), the most potent human estrogen, is known to be involved in the etiology of estrogen-dependent diseases (EDD) like breast cancer and…”
Get full text

Inhibition of 17β-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker by Abdelsamie, Ahmed S., Bey, Emmanuel, Hanke, Nina, Empting, Martin, Hartmann, Rolf W., Frotscher, Martin

“…Estradiol is the most potent estrogen in humans. It is known to be involved in the development and proliferation of estrogen dependent diseases such as breast…”
Get full text

Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases by Bey, Emmanuel, Marchais-Oberwinkler, Sandrine, Kruchten, Patricia, Frotscher, Martin, Werth, Ruth, Oster, Alexander, Algül, Oztekin, Neugebauer, Alexander, Hartmann, Rolf W.

“…A series of 19 azoles were synthesised and 17β-HSD1 inhibition determined. Compound 18 showed highest activity in cell free and T-47D assays, excellent…”
Get full text

Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17β-HSD1 inhibitor with sub-nanomolar IC 50 for a proof-of-principle study by Abdelsamie, Ahmed S, van Koppen, Chris J, Bey, Emmanuel, Salah, Mohamed, Börger, Carsten, Siebenbürger, Lorenz, Laschke, Matthias W, Menger, Michael D, Frotscher, Martin

“…Current endocrine therapeutics for the estrogen-dependent disease endometriosis often lead to considerable side-effects as they act by reducing estrogen action…”
Get full text

Novel estrone mimetics with high 17β-HSD1 inhibitory activity by Oster, Alexander, Klein, Tobias, Werth, Ruth, Kruchten, Patricia, Bey, Emmanuel, Negri, Matthias, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W.

“…Estrone mimetics were synthesized and 17β-HSD1 inhibition was determined. Compound 12 showed high inhibitory activity, selectivity toward 17β-HSD2, ERα/ERβ and…”
Get full text

Substituted 6-Phenyl-2-naphthols. Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Design, Synthesis, Biological Evaluation, and Pharmacokinetics by Marchais-Oberwinkler, Sandrine, Kruchten, Patricia, Frotscher, Martin, Ziegler, Erika, Neugebauer, Alexander, Bhoga, Umadevi, Bey, Emmanuel, Müller-Vieira, Ursula, Messinger, Josef, Thole, Hubert, Hartmann, Rolf W

“…17β-Estradiol (E2) is implicated in the genesis and the development of estrogen-dependent diseases. Its concentration is mainly regulated by 17β-hydroxysteroid…”
Get full text

Selective inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17βHSD1) reduces estrogen responsive cell growth of T47-D breast cancer cells by Kruchten, Patricia, Werth, Ruth, Bey, Emmanuel, Oster, Alexander, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W.

“…The most potent estrogen estradiol (E2) plays a pivotal role in the initiation and progression of estrogen dependent diseases. 17β-Hydroxysteroid dehydrogenase…”
Get full text

Hydroxybenzothiazoles as New Nonsteroidal Inhibitors of 17[beta]-Hydroxysteroid Dehydrogenase Type 1 by Spadaro, Alessandro, Negri, Matthias, Marchais-Oberwinkler, Sandrine, Bey, Emmanuel, Frotscher, Martin

“…17[beta]-estradiol (E2), the most potent estrogen in humans, known to be involved in the development and progession of estrogen-dependent diseases (EDD) like…”
Get full text

The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17β-Hydroxysteroid Dehydrogenase (17β-HSD) type 1 and type 2 by Al-Soud, Yaseen A., Bey, Emmanuel, Oster, Alexander, Marchais-Oberwinkler, Sandrine, Werth, Ruth, Kruchten, Patricia, Frotscher, Martin, Hartmann, Rolf W.

“…17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is responsible for the catalytic reduction of the weak estrogen estrone (E1) into the highly potent…”
Get full text

Aging Reduces the Efficacy of Estrogen Substitution to Attenuate Cardiac Hypertrophy in Female Spontaneously Hypertensive Rats by Jazbutyte, Virginija, Hu, Kai, Kruchten, Patricia, Bey, Emmanuel, Maier, Sebastian K.G, Fritzemeier, Karl-Heinrich, Prelle, Katja, Hegele-Hartung, Christa, Hartmann, Rolf W, Neyses, Ludwig, Ertl, Georg, Pelzer, Theo

“…Clinical trials failed to show a beneficial effect of postmenopausal hormone replacement therapy, whereas experimental studies in young animals reported a…”
Get full text

The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17beta-Hydroxysteroid Dehydrogenase (17beta-HSD) type 1 and type 2 by Al-Soud, Yaseen A, Bey, Emmanuel, Oster, Alexander, Marchais-Oberwinkler, Sandrine, Werth, Ruth, Kruchten, Patricia, Frotscher, Martin, Hartmann, Rolf W

“…17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) is responsible for the catalytic reduction of the weak estrogen estrone (E1) into the highly potent…”
Get full text

Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17p-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases by BEY, Emmanuel, MARCHAIS-OBERWINKLER, Sandrine, KRUCHTEN, Patricia, FROTSCHER, Martin, WERTH, Ruth, OSTER, Alexander, ALGÜL, Oztekin, NEUGEBAUER, Alexander, HARTMANN, Rolf W

Get full text

Novel estrone mimetics with high 17beta-HSD1 inhibitory activity by Oster, Alexander, Klein, Tobias, Werth, Ruth, Kruchten, Patricia, Bey, Emmanuel, Negri, Matthias, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W

“…17Beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the reduction of estrone into estradiol, which is the most potent estrogen in humans…”
Get full text

Aging reduces the efficacy of estrogen substitution to attenuate cardiac hypertrophy in female spontaneously hypertensive rats. Commentary by HINOJOSA-LABORDE, Carmen, LINDSEY, Merry L, HARTMANN, Rolf W, NEYSES, Ludwig, ERTL, Georg, PELZER, Theo, JAZBUTYTE, Virginija, KAI HU, KRUCHTEN, Patricia, BEY, Emmanuel, MAIER, Sebastian K. G, FRITZEMEIER, Karl-Heinrich, PRELLE, Katja, HEGELE-HARTUNG, Christa

Get full text

Selective inhibition of 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) reduces estrogen responsive cell growth of T47-D breast cancer cells by Kruchten, Patricia, Werth, Ruth, Bey, Emmanuel, Oster, Alexander, Marchais-Oberwinkler, Sandrine, Frotscher, Martin, Hartmann, Rolf W

“…The most potent estrogen estradiol (E2) plays a pivotal role in the initiation and progression of estrogen dependent diseases. 17beta-Hydroxysteroid…”
Get full text

New insights into the SAR and binding modes of bis(hydroxyphenyl)thiophenes and -benzenes: influence of additional substituents on 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitory activity and selectivity by Bey, Emmanuel, Marchais-Oberwinkler, Sandrine, Negri, Matthias, Kruchten, Patricia, Oster, Alexander, Klein, Tobias, Spadaro, Alessandro, Werth, Ruth, Frotscher, Martin, Birk, Barbara, Hartmann, Rolf W

“…17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) is responsible for the catalytic reduction of weakly active E1 to highly potent E2. E2 stimulates the…”
Get full text