取代 C19 甾体 17-肟类化合物的合成与芳香酶抑制活性筛选。

College of Pharmacy, Catholic University of Daegu, Hayang, 712-702, Korea.

Molecules. 2011 Nov 28;16(12):9868-85. doi: 10.3390/molecules16129868.

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.

描述了雄甾-4-烯、雄甾-5-烯、1β,2β-环氧-和/或雄甾-4,6-二烯、4β,5β-环氧雄甾烷-和 4-取代的雄甾-4-烯-17-肟衍生物的合成和芳香酶抑制活性。使用芳香酶酶和[1β-3H]雄烯二酮作为底物评估合成化合物的抑制活性。大多数化合物表现出与法倔唑（74.2%）相似或更高的芳香酶抑制活性。4-氯-3β-羟基-4-雄甾-17-酮肟（14，93.8%）表现出最高的活性，而 4-叠氮-3β-羟基-4-雄甾-17-酮肟（17，32.8%）对芳香酶的抑制活性最低。