Document Report Card

ID: ALA3259565

Journal: ACS Med Chem Lett

Title: Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.

Authors: Devkota K, Lohse B, Liu Q, Wang MW, Stærk D, Berthelsen J, Clausen RP.

Abstract: A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.

CiteXplore: 24900829

DOI: 10.1021/ml4002503