Bioorganic and Medicinal Chemistry p. 4579 - 4594 (2017)
Update date:2022-08-29
Topics:
Liu, Qing
Cai, Xiaoqing
Yang, Dehua
Chen, Yi
Wang, Yafang
Shao, Liming
Wang, Ming-Wei
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%, IC50 = 21.8 μM for EHMT1 and 77.6%, IC50 = 39.6 μM for EHMT2, respectively) similar to that of sinefungin (100.0%, IC50 = 28.4 μM for EHMT1 and 79.5%, IC50 = 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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