89593-30-6Relevant articles and documents
Synthesis and evaluation of novel 4-amino-4,6-androstadiene-3,17-dione: An analog of formestane
Sharma, Sanjay K.,Zheng, Weizhong,Joshua, Alummoottil V.,Abrams, Douglas N.,McEwan, Alexander J.B.
, p. 5563 - 5566 (2008)
Synthesis of 4-amino-4,6-androstadiene-3,17-dione 7, an analog of formestane used in breast cancer therapy as an aromatase inhibitor, from 4-acetoxy-4-androstene-3,17-dione 2 is described. This is the first report of a 4-amino diene (4,6) system in this series of molecules. The new (7) and reported molecules were screened by the National Cancer Institute (NCI, Bethesda, USA) for in vitro antitumor activity against 60 human cancer cell lines. Molecule 7 showed best activity against breast cancer cell line (MCF-7).
The Synthesis of 4-Hydroxyandrost-4-ene-3,17-dione and other Potential Aromatase Inhibitors
Mann, John,Pietrzak, Barbara
, p. 2681 - 2685 (2007/10/02)
We describe novel syntheses of 4-hydroxyandrost-4-ene-3,17-dione (Ia) and related compounds, some containing fluorine.In addition we provide further evidence of the general tendency of 2- and 6-substituted androst-4-ene-3,17-diones to undergo rearrangement reactions, and thus provide new routes to 6-fluoro- and 2,6-difluoro-derivatives.Several of these compounds are potent aromatase inhibitors.