Literature DB >> 20030343

Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins).

Kilian Huber1, Jörg Schemies, Urszula Uciechowska, Julia M Wagner, Tobias Rumpf, Felicitas Lewrick, Regine Süss, Wolfgang Sippl, Manfred Jung, Franz Bracher.   

Abstract

Class III histone deacetylases (sirtuins) play pivotal roles in many cellular processes. They are linked to extended lifespan and to the pathogenesis of cancer and neuronal disorders. We present novel sirtuin inhibitors based on a 6,7-dichloro-2-oxindole scaffold with low micromolar activity. In vitro activity was rationalized by docking studies, and hyperacetylation of sirtuin targets could be demonstrated in cell culture.

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Year:  2010        PMID: 20030343     DOI: 10.1021/jm901055u

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  12 in total

1.  3-(N-arylsulfamoyl)benzamides, inhibitors of human sirtuin type 2 (SIRT2).

Authors:  Soo Hyuk Choi; Luisa Quinti; Aleksey G Kazantsev; Richard B Silverman
Journal:  Bioorg Med Chem Lett       Date:  2012-03-03       Impact factor: 2.823

Review 2.  Using mitochondrial sirtuins as drug targets: disease implications and available compounds.

Authors:  Melanie Gertz; Clemens Steegborn
Journal:  Cell Mol Life Sci       Date:  2016-03-23       Impact factor: 9.261

3.  Design of a novel nucleoside analog as potent inhibitor of the NAD dependent deacetylase, SIRT2.

Authors:  Padavattan Sivaraman; Suresh Mattegunta; Gottumukkala V Subbaraju; Chava Satyanarayana; Balasundaram Padmanabhan
Journal:  Syst Synth Biol       Date:  2011-02-23

Review 4.  Sirtuin modulators.

Authors:  Sumit S Mahajan; Vid Leko; Julian A Simon; Antonio Bedalov
Journal:  Handb Exp Pharmacol       Date:  2011

Review 5.  Metabolism as a key to histone deacetylase inhibition.

Authors:  Praveen Rajendran; David E Williams; Emily Ho; Roderick H Dashwood
Journal:  Crit Rev Biochem Mol Biol       Date:  2011-04-05       Impact factor: 8.250

Review 6.  Sirtuin inhibitors as anticancer agents.

Authors:  Jing Hu; Hui Jing; Hening Lin
Journal:  Future Med Chem       Date:  2014-05       Impact factor: 3.808

7.  Discovery of 5-Benzylidene-2-phenyl-1,3-dioxane-4,6-diones as Highly Potent and Selective SIRT1 Inhibitors.

Authors:  Chunpu Li; Sha-Sha Hu; Lisheng Yang; Min Wang; Jian-Dong Long; Bing Wang; Haozhen Han; Haoran Zhu; Sen Zhao; Jing-Gen Liu; Dongxiang Liu; Hong Liu
Journal:  ACS Med Chem Lett       Date:  2021-03-01       Impact factor: 4.345

Review 8.  Rejuvenating sirtuins: the rise of a new family of cancer drug targets.

Authors:  Santina Bruzzone; Marco Daniele Parenti; Alessia Grozio; Alberto Ballestrero; Inga Bauer; Alberto Del Rio; Alessio Nencioni
Journal:  Curr Pharm Des       Date:  2013       Impact factor: 3.116

9.  The gramine route to pyrido[4,3-b]indol-3-ones - identification of a new cytotoxic lead.

Authors:  Uwe Wollein; Franz Bracher
Journal:  Sci Pharm       Date:  2010-12-18

10.  Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.

Authors:  Oleg Fedorov; Kilian Huber; Andreas Eisenreich; Panagis Filippakopoulos; Oliver King; Alex N Bullock; Damian Szklarczyk; Lars J Jensen; Doriano Fabbro; Jörg Trappe; Ursula Rauch; Franz Bracher; Stefan Knapp
Journal:  Chem Biol       Date:  2011-01-28
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