Synthesis of 10 beta-(1'-azirinyl)estr-4-en-3,17-dione as an aromatase inhibitor

被引：9
|
作者：
Njar, VCO [1 ]
Duerkop, J [1 ]
Hartmann, RW [1 ]
机构：
[1] UNIV SAARLAND,FACHRICHTUNG 12,D-66041 SAARBRUCKEN,GERMANY
来源：
STEROIDS | 1996年 / 61卷 / 03期
关键词：
10 beta-1'-azirinyl steroid; aromatase inhibitor; synthesis;
D O I：
10.1016/0039-128X(95)00217-E
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The novel 10 beta-(1'-azirinyl)estr-4-en-3,17-dione (10) has been synthesized from 19-methyl-19-methiodide salt intermediates 15 and 16 by a modified Neber reaction. Four other hitherto undescribed 10 beta-1'-azirinyl steroids 9, 12, 17, and 18 were also synthesized. Compound 10 inhibited human placental aromatase in vitro (IC50 value = 5.5 mu M) but was not as potent as the related (19R)-10 beta-aziridine (1).
引用
收藏
页码：138 / 143
页数：6
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