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Synthesis and screening of aromatase inhibitory activity of substituted C19 steroidal 17-oxime analogs.

ABSTRACT: The synthesis and aromatase inhibitory activity of androst-4-en-, androst-5-en-, 1?,2?-epoxy- and/or androsta-4,6-dien-, 4?,5?-epoxyandrostane-, and 4-substituted androst-4-en-17-oxime derivatives are described. Inhibition activity of synthesized compounds was assessed using aromatase enzyme and [1?-3H]androstenedione as substrate. Most of the compounds displayed similar to or more aromatase inhibitory activity than formestane (74.2%). 4-Chloro-3?-hydroxy-4-androsten-17-one oxime (14, 93.8%) showed the highest activity, while 4-azido-3?-hydroxy-4-androsten-17-one oxime (17, 32.8%) showed the lowest inhibitory activity for aromatase.

SUBMITTER: Pokhrel M

PROVIDER: S-EPMC6264551 | biostudies-literature | 2011 Nov

REPOSITORIES: biostudies-literature

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Synthesis and screening of aromatase inhibitory activity of substituted C19 steroidal 17-oxime analogs.

Pokhrel Muna M Ma Eunsook E

Molecules (Basel, Switzerland) 20111128 12

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%) sho ...[more]

PMID: 22124202

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