Estrone C15 derivatives—A new class of 17β-hydroxysteroid dehydrogenase type 1 inhibitors

Anticancer effects of estrone derivatives and nonsteroidal 17β- hydroxysteroid dehydrogenase type 1 inhibitors

s: I. Wölfling J, Bóna Á, Frank É, Schneider G, Berényi Á, Zupkó I. Synthesis and cytotoxic activity of 16-benzylidene estrone 3-methyl ethers. Hungarian-AustrianCzech-German-Greek-Italian-Polish-Slovak-Slovenian Joint Meeting on Medicinal Chemistry, 24-27. June, 2009, Budapest, Hungary. II. Zupkó I, Berényi Á, Marchais-Oberwinkler S, Frotscher M. Direct antiproliferative effect of novel nonste...

Hydroxybenzothiazoles as New Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1)

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 cancer and endometriosis. 17β-HSD1, which catalyses the reduction of the weak estrogen estrone (E1) to E2, is often overexpressed in breast cancer and endometriotic tissues. An inhibition of 17β-HSD1 could selectively reduce the local E2...

Anticancer Effects of Estrone Derivatives and Nonsteroidal 17β-hydroxysteroid Dehydrogenase Inhibitors

Synthesis and Molecular Docking Studies of 2-arylideneindan-1,3-diones Derivatives as an Inhibitor of 17β-hydroxysteroid Dehydrogenase Type 1

Due to the drawbacks of applying catalysts in the synthesis of α,β-unsaturated structure units and the importance of these materials, electrochemistry has been introduced as an efficient alternative.Therefore, herein a high-yield synthesis of 2-arylideneindan-1,3-diones is proposed. The procedure is carried out in propanol, using electrons as a green catalyst for generating propanol anion...

Roles of 17β-hydroxysteroid dehydrogenase type 10 in neurodegenerative disorders

17β-Hydroxysteroid dehydrogenase type 10 (17β-HSD10) is encoded by the HSD17B10 gene mapping at Xp11.2. This homotetrameric mitochondrial multifunctional enzyme catalyzes the oxidation of neuroactive steroids and the degradation of isoleucine. This enzyme is capable of binding to other peptides, such as estrogen receptor α, amyloid-β, and tRNA methyltransferase 10C. Missense mutations of the HS...