Anticancer Effects of Estrone Derivatives and Nonsteroidal 17β-hydroxysteroid Dehydrogenase Inhibitors
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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...
متن کاملAnticancer 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...
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17β-Hydroxysteroid dehydrogenase 2 (17β-HSD2) catalyzes the inactivation of estradiol into estrone. This enzyme is expressed only in a few tissues, and therefore its inhibition is considered as a treatment option for osteoporosis to ameliorate estrogen deficiency. In this study, ligand-based pharmacophore models for 17β-HSD2 inhibitors were constructed and employed for virtual screening. From t...
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Novel 13α-estrone derivatives were synthesized by Sonogashira coupling. Transformations of 2- or 4-iodo regioisomers of 13α-estrone and its 3-methyl ether were carried out under different conditions in a microwave reactor. The 2-iodo isomers were reacted with para-substituted phenylacetylenes using Pd(PPh3)4 as catalyst and CuI as a cocatalyst. Coupling reactions of 4-iodo derivatives could be ...
متن کاملHydroxybenzothiazoles 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...
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تاریخ انتشار 2013