Search Results - "Kruchten, Patricia"
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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
Published in Journal of medicinal chemistry (12-11-2009)“…17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is responsible for the catalytic reduction of weakly active E1 to highly potent E2. E2 stimulates the…”
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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)
Published in Journal of medicinal chemistry (13-11-2008)“…17β-Estradiol (E2), the most potent female sex hormone, stimulates the growth of mammary tumors and endometriosis via activation of the estrogen receptor α…”
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New Drug-Like Hydroxyphenylnaphthol Steroidomimetics As Potent and Selective 17β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors for the Treatment of Estrogen-Dependent Diseases
Published in Journal of medicinal chemistry (27-01-2011)“…Inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a novel and attractive approach to reduce the local levels of the active estrogen…”
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Development of a biological screening system for the evaluation of highly active and selective 17β-HSD1-inhibitors as potential therapeutic agents
Published in Molecular and cellular endocrinology (25-03-2009)“…17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the intracellular conversion of oestrone (E1) to oestradiol (E2). E2 is known to be involved in…”
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Design, Synthesis, and Biological Evaluation of (Hydroxyphenyl)naphthalene and -quinoline Derivatives: Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) for the Treatment of Estrogen-Dependent Diseases
Published in Journal of medicinal chemistry (10-04-2008)“…Human 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the reduction of the weak estrogen estrone (E1) to the highly potent estradiol (E2). This…”
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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
Published in Bioorganic & medicinal chemistry (15-06-2008)“…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…”
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Novel estrone mimetics with high 17β-HSD1 inhibitory activity
Published in Bioorganic & medicinal chemistry (15-05-2010)“…Estrone mimetics were synthesized and 17β-HSD1 inhibition was determined. Compound 12 showed high inhibitory activity, selectivity toward 17β-HSD2, ERα/ERβ and…”
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Substituted 6-Phenyl-2-naphthols. Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Design, Synthesis, Biological Evaluation, and Pharmacokinetics
Published in Journal of medicinal chemistry (14-08-2008)“…17β-Estradiol (E2) is implicated in the genesis and the development of estrogen-dependent diseases. Its concentration is mainly regulated by 17β-hydroxysteroid…”
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Selective inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17βHSD1) reduces estrogen responsive cell growth of T47-D breast cancer cells
Published in The Journal of steroid biochemistry and molecular biology (01-04-2009)“…The most potent estrogen estradiol (E2) plays a pivotal role in the initiation and progression of estrogen dependent diseases. 17β-Hydroxysteroid dehydrogenase…”
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Structure–activity study in the class of 6-(3′-hydroxyphenyl)naphthalenes leading to an optimization of a pharmacophore model for 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) inhibitors
Published in Molecular and cellular endocrinology (25-03-2009)“…17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the transformation of estrone (E1) into the most potent estrogen, estradiol (E2), which stimulates…”
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The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17β-Hydroxysteroid Dehydrogenase (17β-HSD) type 1 and type 2
Published in Molecular and cellular endocrinology (25-03-2009)“…17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is responsible for the catalytic reduction of the weak estrogen estrone (E1) into the highly potent…”
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12
Development of a biological screening system for the evaluation of highly active and selective 17beta-HSD1-inhibitors as potential therapeutic agents
Published in Molecular and cellular endocrinology (25-03-2009)“…17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyses the intracellular conversion of oestrone (E1) to oestradiol (E2). E2 is known to be involved…”
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Aging Reduces the Efficacy of Estrogen Substitution to Attenuate Cardiac Hypertrophy in Female Spontaneously Hypertensive Rats
Published in Hypertension (Dallas, Tex. 1979) (01-10-2006)“…Clinical trials failed to show a beneficial effect of postmenopausal hormone replacement therapy, whereas experimental studies in young animals reported a…”
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Structure-activity study in the class of 6-(3'-hydroxyphenyl)naphthalenes leading to an optimization of a pharmacophore model for 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) inhibitors
Published in Molecular and cellular endocrinology (25-03-2009)“…17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the transformation of estrone (E1) into the most potent estrogen, estradiol (E2), which…”
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The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17beta-Hydroxysteroid Dehydrogenase (17beta-HSD) type 1 and type 2
Published in Molecular and cellular endocrinology (25-03-2009)“…17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) is responsible for the catalytic reduction of the weak estrogen estrone (E1) into the highly potent…”
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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
Published in Bioorganic & medicinal chemistry (2008)Get full text
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Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases
Published in Journal of medicinal chemistry (10-04-2008)“…Human 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the reduction of the weak estrogen estrone (E1) to the highly potent estradiol (E2)…”
Get full text
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Novel estrone mimetics with high 17beta-HSD1 inhibitory activity
Published in Bioorganic & medicinal chemistry (15-05-2010)“…17Beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the reduction of estrone into estradiol, which is the most potent estrogen in humans…”
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