Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
Basic Information
ID: ALA4043120
Journal: Bioorg Med Chem
Title: Cycloalkane analogues of sinefungin as EHMT1/2 inhibitors.
Authors: Liu Q, Cai X, Yang D, Chen Y, Wang Y, Shao L, Wang MW.
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%, IC50=21.8μM for EHMT1 and 77.6%, IC50=39.6μM for EHMT2, respectively) similar to that of sinefungin (100.0%, IC50=28.4μM for EHMT1 and 79.5%, IC50=30.1μM for EHMT2, respectively). Further studies against other methyltransferases such as PRMT1 showed no activity except that 12d displayed about 20% inhibition.
CiteXplore: 28739157
DOI: 10.1016/j.bmc.2017.06.032
Patent ID: ┄