1078734-20-9Relevant academic research and scientific papers
17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
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Page/Page column 26, (2011/04/14)
The invention relates to 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) inhibitors, the preparation thereof and the use thereof for the treatment and prophylaxis of hormone-related, especially estrogen-related or androgen-related, diseases.
Preparation of polyfunctional zinc organometallics using an Fe- or Co-catalyzed Cl/Zn-exchange
Melzig, Laurin,Diene, Coura R.,Rohbogner, Christoph J.,Knochel, Paul
, p. 3174 - 3177 (2011/08/06)
A new Fe- or Co-catalyzed Cl/Zn-exchange reaction allows the direct transformation of aryl, heteroaryl, and also alkyl chlorides into the corresponding zinc reagents. The method tolerates functional groups such as a nitrile or an ester. Remarkably, secondary and tertiary alkyl chlorides are suitable substrates for the Cl/Zn exchange.
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
Bey, Emmanuel,Marchais-Oberwinkler, Sandrine,Negri, Matthias,Kruchten, Patricia,Oster, Alexander,Klein, Tobias,Spadaro, Alessandro,Werth, Ruth,Frotscher, Martin,Birk, Barbara,Hartmann, Rolf W.
experimental part, p. 6724 - 6743 (2010/04/05)
17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is responsible for the catalytic reduction of weakly active E1 to highly potent E2. E2 stimulates the proliferation of hormone-dependent diseases via activation of the estrogen receptor α (ERα). Because o
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)
Bey, Emmanuel,Marchais-Oberwinkler, Sandrine,Werth, Ruth,Negri, Matthias,Al-Soud, Yaseen A.,Kruchten, Patricia,Oster, Alexander,Frotscher, Martin,Birk, Barbara,Hartmann, Rolf W.
experimental part, p. 6725 - 6739 (2009/11/30)
17β-Estradiol (E2), the most potent female sex hormone, stimulates the growth of mammary tumors and endometriosis via activation of the estrogen receptor α (ERα). 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1), which is responsible for the catalytic r
