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

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

College of Pharmacy, Catholic University of Daegu, Hayang, 712-702, Korea
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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 (CC BY 3.0).

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MDPI and ACS Style

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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