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Molecules 2011, 16(12), 9868-9885; doi:10.3390/molecules16129868
Article

Synthesis and Screening of Aromatase Inhibitory Activity of Substituted C19 Steroidal 17-Oxime Analogs

 and *
Received: 7 October 2011 / Revised: 5 November 2011 / Accepted: 7 November 2011 / Published: 28 November 2011
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Abstract

The synthesis and aromatase inhibitory activity of androst-4-en-, androst-5-en-, 1β,2β-epoxy- and/or androsta-4,6-dien-, 4β,5β-epoxyandrostane-, and 4-substituted androst-4-en-17-oxime derivatives are described. Inhibition activity of synthesized compounds was assessed using aromatase enzyme and [1β-3H]androstenedione as substrate. Most of the compounds displayed similar to or more aromatase inhibitory activity than formestane (74.2%). 4-Chloro-3β-hydroxy-4-androsten-17-one oxime (14, 93.8%) showed the highest activity, while 4-azido-3β-hydroxy-4-androsten-17-one oxime (17, 32.8%) showed the lowest inhibitory activity for aromatase.
Keywords: aromatase inhibitor; breast cancer; conjugated androstadiene-17-oxime; 4-substituted androstene-17-oxime aromatase inhibitor; breast cancer; conjugated androstadiene-17-oxime; 4-substituted androstene-17-oxime
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Pokhrel, M.; Ma, E. Synthesis and Screening of Aromatase Inhibitory Activity of Substituted C19 Steroidal 17-Oxime Analogs. Molecules 2011, 16, 9868-9885.

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