Synthesis and estrogenic activities of novel 7-thiosubstituted estratriene derivatives
β Scribed by Chris P. Miller; Ivo Jirkovsky; Bach D. Tran; Heather A. Harris; Robert A. Moran; Barry S. Komm
- Book ID
- 104364931
- Publisher
- Elsevier Science
- Year
- 2000
- Tongue
- English
- Weight
- 144 KB
- Volume
- 10
- Category
- Article
- ISSN
- 0960-894X
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β¦ Synopsis
AbstractΓA diastereomerically pure series of 7a-thioestratrienes was prepared and evaluated for its anity for both the human estrogen receptor a and the more recently discovered estrogen receptor b. The functional estrogenic activities of the compounds were measured in a MCF-7 ERE-tk-luciferase assay. The activities and selectivities of the compounds were sensitive to the nature of the thioether side chain.
π SIMILAR VOLUMES
The starting compound for synthesis of new 16,17-seco-estratriene derivatives was 3-benzyloxy-17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile (1b), obtained from estrone in several synthetic steps. 17-Tosyl, -chloro-, bromo-, and -iodo-derivatives 2b, 4b, 5b, and 6b were prepared directly fro