1078733-86-4Relevant academic research and scientific papers
Pseudo five-component synthesis of 2,5-di(hetero)arylthiophenes via a one-pot Sonogashira-Glaser cyclization sequence
Urselmann, Dominik,Antovic, Dragutin,Mueller, Thomas J. J.
, p. 1499 - 1503 (2011/12/22)
Based upon a consecutive one-pot Sonogashira-Glaser coupling-cyclization sequence a variety of 2,5-di(hetero)arylthiophenes were synthesized in moderate to good yields. A single Pd/Cu-catalyst system, without further catalyst addition, and easily available, stable starting materials were used, resulting in a concise and highly efficient route for the synthesis of the title compounds. This novel pseudo five-component synthesis starting from iodo(hetero)arenes is particularly suitable as a direct access to well-defined thiophene oligomers, which are of peculiar interest in materials science.
17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
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Page/Page column 28, (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.
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.
scheme or table, 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
