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

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.

SUBMITTER: Devkota K

PROVIDER: S-EPMC4027773 | biostudies-literature | 2014 Apr

REPOSITORIES: biostudies-literature

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

Devkota Kanchan K Lohse Brian B Liu Qing Q Wang Ming-Wei MW Stærk Dan D Berthelsen Jens J Clausen Rasmus Prætorius RP

ACS medicinal chemistry letters 20140131 4

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. ...[more]

PMID: 24900829

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