Design, synthesis, inhibitory activity, and binding mode study of novel DNA methyltransferase 1 inhibitors

Copyright (c) 2009 Elsevier Ltd. All rights reserved..

To identify novel non-nucleoside DNA methyltransferase (DNMT) inhibitors, we designed and synthesized a series of maleimide derivatives. Among this series, compounds 5-8 were found to be more potent DNMT1 inhibitors than RG108, a DNMT1 inhibitor reported previously by Siedlecki et al. The binding mode analysis of compound 5 is also reported.

Medienart:

E-Artikel

Erscheinungsjahr:

2010

Erschienen:

2010

Enthalten in:

Zur Gesamtaufnahme - volume:20

Enthalten in:

Bioorganic & medicinal chemistry letters - 20(2010), 3 vom: 01. Feb., Seite 1124-7

Sprache:

Englisch

Beteiligte Personen:

Suzuki, Takayoshi [VerfasserIn]
Tanaka, Rikako [VerfasserIn]
Hamada, Shohei [VerfasserIn]
Nakagawa, Hidehiko [VerfasserIn]
Miyata, Naoki [VerfasserIn]

Links:

Volltext

Themen:

8DUH1N11BX
Comparative Study
DNA (Cytosine-5-)-Methyltransferase 1
DNA (Cytosine-5-)-Methyltransferases
DNMT1 protein, human
EC 2.1.1.37
Indoles
Journal Article
Maleimides
Phthalimides
Propionates
RG108
Research Support, Non-U.S. Gov't
Tryptophan

Anmerkungen:

Date Completed 20.09.2010

Date Revised 16.11.2017

published: Print-Electronic

Citation Status MEDLINE

doi:

10.1016/j.bmcl.2009.12.016

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM194191249