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

Molecules

Muna Pokhrel¹ 

[1] College of Pharmacy, Catholic University of Daegu, Hayang, 712-702, Korea

关键词: aromatase inhibitor;    breast cancer;    conjugated androstadiene-17-oxime;    4-substituted androstene-17-oxime;   

DOI  :  10.3390/molecules16129868

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.