Patricia Kruchten

No ORCID on file · 7 papers in corpus
lab-animal 2011
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases
Journal of medicinal chemistry ·doi:10.1021/jm1009082

Inhibition of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a novel and attractive approach to reduce the local levels of the active estrogen 17β-estradiol in patients with estrogen-dependent diseases like breast cancer or endometri…

lab-animal 2010
Novel estrone mimetics with high 17beta-HSD1 inhibitory activity
Bioorganic & medicinal chemistry ·doi:10.1016/j.bmc.2010.03.065

17Beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the reduction of estrone into estradiol, which is the most potent estrogen in humans. Lowering intracellular estradiol concentration by inhibition of this enzyme is a promis…

lab-animal 2009
Development of a biological screening system for the evaluation of highly active and selective 17beta-HSD1-inhibitors as potential therapeutic agents
Molecular and cellular endocrinology ·doi:10.1016/j.mce.2008.09.035

17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyses the intracellular conversion of oestrone (E1) to oestradiol (E2). E2 is known to be involved in the development and progression of breast cancer and endometriosis. Since 17b…

lab-animal 2009
Selective inhibition of 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) reduces estrogen responsive cell growth of T47-D breast cancer cells
The Journal of steroid biochemistry and molecular biology ·doi:10.1016/j.jsbmb.2009.02.006

The most potent estrogen estradiol (E2) plays a pivotal role in the initiation and progression of estrogen dependent diseases. 17beta-Hydroxysteroid dehydrogenase type 1 (17betaHSD1) catalyses the NADPH-dependent E2-formation from estrone (…

lab-animal 2009
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
Molecular and cellular endocrinology ·doi:10.1016/j.mce.2008.09.024

17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) catalyzes the transformation of estrone (E1) into the most potent estrogen, estradiol (E2), which stimulates cell proliferation and decreases apoptosis. 17beta-HSD1 is often strongly …

lab-animal 2009
The role of the heterocycle in bis(hydroxyphenyl)triazoles for inhibition of 17beta-Hydroxysteroid Dehydrogenase (17beta-HSD) type 1 and type 2
Molecular and cellular endocrinology ·doi:10.1016/j.mce.2008.09.012

17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1) is responsible for the catalytic reduction of the weak estrogen estrone (E1) into the highly potent 17beta-estradiol (E2). As 17beta-HSD1 is often overexpressed in mammary tumors and …

lab-animal 2008
Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1)
Journal of medicinal chemistry ·doi:10.1021/jm8006917

17beta-Estradiol (E2), the most potent female sex hormone, stimulates the growth of mammary tumors and endometriosis via activation of the estrogen receptor alpha (ERalpha). 17beta-Hydroxysteroid dehydrogenase type 1 (17beta-HSD1), which is…