Total Synthesis of (+)-Chaetocin and its Analogues: Their Histone Methyltransferase G9a Inhibitory Activity

Iwasa, Eriko; Hamashima, Yoshitaka; Fujishiro, Shinya; Higuchi, Eisuke; Ito, Akihiro; Yoshida, Minoru; Sodeoka, Mikiko

doi:10.1021/ja101280p

Public

Total Synthesis of (+)-Chaetocin and its Analogues: Their Histone Methyltransferase G9a Inhibitory Activity

Published in Journal of the American Chemical Society • Mar 8, 2010

Authors:

Eriko Iwasa

Yoshitaka Hamashima

Shinya Fujishiro

Abstract

The first total synthesis of (+)-chaetocin has been accomplished in nine steps starting from known N-Cbz-N-Me-serine using radical alpha-bromination reaction of diketopiperazine 10 and Co(I)-mediated reductive dimerization reaction of 12 as key reactions. The enantiomers show comparable inhibitory a...

Subject

Chemistry

Inhibitory postsynaptic potential

Halogenation

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