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

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 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...

Structural Basis for Species Specific Inhibition of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1): Computational Study and Biological Validation

17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the reduction of estrone to estradiol, which is the most potent estrogen in humans. Inhibition of 17β-HSD1 and thereby reducing the intracellular estradiol concentration is thus a promising approach for the treatment of estrogen dependent diseases. In the past, several steroidal and non-steroidal inhibitors of 17β-HSD1 have been descr...

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...

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