Probing the Hydrophobic Pocket of the Active Site of Aromatase with 4-Phenoxy-7α-(phenylthio)-4-androstene-3,17-dione

Xing Ping Liu, Didier M. Lambert, Yusuf J Abul-Hajj

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In order to examine the nature of the hydrophobic pocket at the active site of aromatase, we carried out the synthesis, biochemical evaluation, and molecular modeling studies on 4-phenoxy-7α-(phenylthio)-4-androstenedione 2. Aromatase inhibitory activity of 2 was found to be significantly weaker than that of the 4- and 7α-mono(phenylthio)-substituted derivatives of androstenedione. These results along with those obtained from the modeling studies suggest the existence of a single hydrophobic pocket corresponding to the α-face in the C4, C6, C7 region of androstenedione.

Original languageEnglish (US)
Pages (from-to)4135-4138
Number of pages4
JournalJournal of medicinal chemistry
Issue number20
StatePublished - Sep 1 1995


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