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

College of Pharmacy, Catholic University of Daegu, Hayang, 712-702, Korea
* Author to whom correspondence should be addressed.
Received: 7 October 2011; in revised form: 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

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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.

AMA Style

Pokhrel M, Ma E. Synthesis and Screening of Aromatase Inhibitory Activity of Substituted C19 Steroidal 17-Oxime Analogs. Molecules. 2011; 16(12):9868-9885.

Chicago/Turabian Style

Pokhrel, Muna; Ma, Eunsook. 2011. "Synthesis and Screening of Aromatase Inhibitory Activity of Substituted C19 Steroidal 17-Oxime Analogs." Molecules 16, no. 12: 9868-9885.

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