Synthesis and biological evaluation of novel cyclosporin A analogues: Potential soft drugs for the treatment of autoimmune diseases

被引:23
作者
Lazarova, T [1 ]
Chen, JS [1 ]
Hamann, B [1 ]
Kang, JM [1 ]
Hoinuth-Trombino, D [1 ]
Han, F [1 ]
Hoffmann, E [1 ]
McClure, C [1 ]
Eckstein, J [1 ]
Or, YS [1 ]
机构
[1] Enanta Pharmaceut, Watertown, MA 02472 USA
关键词
D O I
10.1021/jm025595i
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Cyclosporin A is effective in the treatment of asthma patients, but its chronic use is limited by toxicity. Novel cyclosporin A analogues were synthesized utilizing the olefin metathesis reaction and evaluated in a calcineurin A inhibition assay. The novel analogues demonstrated activity comparable to activity of the parent molecule and are potential soft drugs.
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收藏
页码:674 / 676
页数:3
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