Analogues of the natural product Sinefungin as inhibitors of EHMT1 and EHMT2

TY - JOUR

T1 - Analogues of the natural product Sinefungin as inhibitors of EHMT1 and EHMT2

AU - Devkota, Kanchan

AU - Lohse, Brian

AU - Liu, Qing

AU - Wang, Ming-Wei

AU - Stærk, Dan

AU - Berthelsen, Jens

AU - Clausen, Rasmus Prætorius

PY - 2014/4/10

Y1 - 2014/4/10

N2 - 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.

AB - 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.

U2 - 10.1021/ml4002503

DO - 10.1021/ml4002503

M3 - Letter

C2 - 24900829

SN - 1948-5875

VL - 5

SP - 293

EP - 297

JO - A C S Medicinal Chemistry Letters

JF - A C S Medicinal Chemistry Letters

IS - 4

ER -