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Literature DB >> 26810607

Rational design and diversity-oriented synthesis of peptoid-based selective HDAC6 inhibitors.

D Diedrich¹, A Hamacher¹, C G W Gertzen¹, L A Alves Avelar¹, G J Reiss², T Kurz¹, H Gohlke¹, M U Kassack¹, F K Hansen¹.

Abstract

A mini library of HDAC inhibitors with peptoid-based cap groups was synthesized using an efficient multicomponent approach. Four compounds were identified as potent HDAC6 inhibitors with a selectivity over other HDAC isoforms. The most potent HDAC6 inhibitor revealed remarkable chemosensitizing properties and completely reverted the cisplatin resistance in Cal27 CisR cells.

Entities: Chemical Gene

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Year: 2016 PMID： 26810607 DOI： 10.1039/c5cc10301k

Source DB: PubMed Journal: Chem Commun (Camb) ISSN： 1359-7345 Impact factor: 6.222

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Cited

11 in total

1. Multicomponent Synthesis and Binding Mode of Imidazo[1,2- a]pyridine-Capped Selective HDAC6 Inhibitors.

Authors: Marcel K W Mackwitz; Alexandra Hamacher; Jeremy D Osko; Jana Held; Andrea Schöler; David W Christianson; Matthias U Kassack; Finn K Hansen
Journal: Org Lett Date: 2018-05-23 Impact factor: 6.005

2. Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity.

Authors: Nicholas J Porter; Jeremy D Osko; Daniela Diedrich; Thomas Kurz; Jacob M Hooker; Finn K Hansen; David W Christianson
Journal: J Med Chem Date: 2018-08-17 Impact factor: 7.446

3. Multicomponent Synthesis, Binding Mode, and Structure-Activity Relationship of Selective Histone Deacetylase 6 (HDAC6) Inhibitors with Bifurcated Capping Groups.

Authors: Nina Reßing; Melf Sönnichsen; Jeremy D Osko; Andrea Schöler; Julian Schliehe-Diecks; Alexander Skerhut; Arndt Borkhardt; Julia Hauer; Matthias U Kassack; David W Christianson; Sanil Bhatia; Finn K Hansen
Journal: J Med Chem Date: 2020-09-01 Impact factor: 7.446

Review 4. Histone Deacetylase Inhibitors: A Prospect in Drug Discovery.

Authors: Rakesh Yadav; Pooja Mishra; Divya Yadav
Journal: Turk J Pharm Sci Date: 2018-12-31

5. Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity.

Authors: Nina Reßing; Viktoria Marquardt; Christoph G W Gertzen; Andrea Schöler; Alexander Schramm; Thomas Kurz; Holger Gohlke; Achim Aigner; Marc Remke; Finn K Hansen
Journal: Medchemcomm Date: 2018-10-23 Impact factor: 3.597

6. One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites.

Authors: Daniela Diedrich; Katharina Stenzel; Eva Hesping; Yevgeniya Antonova-Koch; Tamirat Gebru; Sandra Duffy; Gillian Fisher; Andrea Schöler; Stephan Meister; Thomas Kurz; Vicky M Avery; Elizabeth A Winzeler; Jana Held; Katherine T Andrews; Finn K Hansen
Journal: Eur J Med Chem Date: 2018-09-07 Impact factor: 6.514

7. Structure-Activity and Structure-Toxicity Relationships of Peptoid-Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity.

Authors: Marcel K W Mackwitz; Eva Hesping; Yevgeniya Antonova-Koch; Daniela Diedrich; Tamirat Gebru Woldearegai; Tina Skinner-Adams; Mary Clarke; Andrea Schöler; Laura Limbach; Thomas Kurz; Elizabeth A Winzeler; Jana Held; Katherine T Andrews; Finn K Hansen
Journal: ChemMedChem Date: 2019-02-19 Impact factor: 3.466