Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors

Qing Liu; Xiaoqing Cai; Dehua YangYi ChenYafang WangLiming ShaoMing-Wei Wang

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Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors

机译：Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors

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Graphical abstract Display Omitted Abstract A series of cycloalkyl substituted analogues of the natural product sinefungin lacking the amino-acid moiety was designed and synthesized. Two stereoisomers (6- R and 6- S ) were separated and their bioactivities examined against EHMT1/2. Of which, compound 14d showed an inhibitory activity against EHMT1/2 (88.9, IC 50 = 21.8 μM for EHMT1 and 77.6, IC 50 = 39.6 μM for EHMT2, respectively) similar to that of sinefungin (100.0, IC 50 = 28.4 μM for EHMT1 and 79.5, IC 50 = 30.1 μM for EHMT2, respectively). Further studies against other methyltransferases such as PRMT1 showed no activity except that 12d displayed about 20 inhibition. >

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来源
《Bioorganic and medicinal chemistry》 |2017年第17期|4579-4594|共16页
作者
Qing Liu; Xiaoqing Cai; Dehua YangYi ChenYafang WangLiming ShaoMing-Wei Wang;
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作者单位

School of Pharmacy, Fudan University;

The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy;

Shanghai Institute of Materia Medica, Chinese Academy of Sciences;

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正文语种英语
中图分类药学;
关键词
Methyltransferase inhibitor; Cycloalkyl substituted analogue; Natural product; Sinefungin;

Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors

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