95589-97-2Relevant articles and documents
7α-Substituted Derivatives of Androstenedione as Inhibitors of Estrogen Biosynthesis
Darby, M. V.,Lovett, J. A.,Brueggemeier, R. W.,Groziak, M. P.,Counsell, R. E.
, p. 803 - 807 (2007/10/02)
In an effort to obtain more information on the structure-activity relationship among the 7α-(phenylthio)androstenedione inhibitors of the enzyme aromatase, a series of compounds containing both electron-donating and electron-withdrawing ring substituents was synthesized and tested for aromatase inhibitory activity.No linear correlation between substituent electronic effects and inhibitory activity was observed.The halogen-containing compounds, particularly 8, appeared to be quite potent inhibitors.The 125I analogue of 8 was synthesized in order to evaluate the possibility of side-chain elimination under the assay conditions.Approximately 90percent of -8 remainded intact for up to 1 h under assay conditions.
