Literature DB >> 24944733

Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors.

Fei Chen1, Hui Chai1, Ming-Bo Su1, Yang-Ming Zhang1, Jia Li1, Xin Xie1, Fa-Jun Nan1.   

Abstract

Inspired by the thiazole-thiazoline cap group in natural product largazole, a series of structurally simplified bisthiazole-based histone deacetylase inhibitors were prepared and evaluated. Compound 8f was evaluated in vivo in an experimental autoimmune encephalomyelitis (EAE) model and found to be orally efficacious in ameliorating clinical symptoms of EAE mice.

Entities:  

Keywords:  Histone deacetylase inhibitors; bisthiazole; largazole

Year:  2014        PMID： 24944733      PMCID： PMC4060935          DOI： 10.1021/ml400470s

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  50 in total

1.  Synthesis and biological activity of largazole and derivatives.

Authors:  Tobias Seiser; Faustin Kamena; Nicolai Cramer
Journal:  Angew Chem Int Ed Engl       Date:  2008       Impact factor: 15.336

2.  Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.

Authors:  Hanae Benelkebir; Sabrina Marie; Annette L Hayden; Jason Lyle; Paul M Loadman; Simon J Crabb; Graham Packham; A Ganesan
Journal:  Bioorg Med Chem       Date:  2011-02-17       Impact factor: 3.641

3.  Histone deacetylase inhibitors for treating a spectrum of diseases not related to cancer.

Authors:  Charles A Dinarello; Gianluca Fossati; Paolo Mascagni
Journal:  Mol Med       Date:  2011-05-05       Impact factor: 6.354

4.  HDAC inhibitors as anti-inflammatory agents.

Authors:  I M Adcock
Journal:  Br J Pharmacol       Date:  2007-02-26       Impact factor: 8.739

Review 5.  HDAC inhibitors: modulating leukocyte differentiation, survival, proliferation and inflammation.

Authors:  Matthew J Sweet; Melanie R Shakespear; Nabilah A Kamal; David P Fairlie
Journal:  Immunol Cell Biol       Date:  2011-10-25       Impact factor: 5.126

6.  Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.

Authors:  José A Souto; Esther Vaz; Ilaria Lepore; Ann-Christin Pöppler; Gianluigi Franci; Rosana Alvarez; Lucia Altucci; Angel R de Lera
Journal:  J Med Chem       Date:  2010-06-24       Impact factor: 7.446

Review 7.  Romidepsin for the treatment of cutaneous T-cell lymphoma.

Authors:  Clara Campas-Moya
Journal:  Drugs Today (Barc)       Date:  2009-11       Impact factor: 2.245

8.  Multiple sclerosis: re-expression of a developmental pathway that restricts oligodendrocyte maturation.

Authors:  Gareth R John; Sai Latha Shankar; Bridget Shafit-Zagardo; Aldo Massimi; Sunhee C Lee; Cedric S Raine; Celia F Brosnan
Journal:  Nat Med       Date:  2002-09-23       Impact factor: 53.440

9.  Total synthesis and molecular target of largazole, a histone deacetylase inhibitor.

Authors:  Yongcheng Ying; Kanchan Taori; Hyoungsu Kim; Jiyong Hong; Hendrik Luesch
Journal:  J Am Chem Soc       Date:  2008-05-29       Impact factor: 15.419

10.  Synthesis and conformation-activity relationships of the peptide isosteres of FK228 and largazole.

Authors:  Albert A Bowers; Thomas J Greshock; Nathan West; Guillermina Estiu; Stuart L Schreiber; Olaf Wiest; Robert M Williams; James E Bradner
Journal:  J Am Chem Soc       Date:  2009-03-04       Impact factor: 15.419
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  5 in total

1.  Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue.

Authors:  Jehad Almaliti; Ayad A Al-Hamashi; Ahmed T Negmeldin; Christin L Hanigan; Lalith Perera; Mary Kay H Pflum; Robert A Casero; L M Viranga Tillekeratne
Journal:  J Med Chem       Date:  2016-11-21       Impact factor: 7.446

Review 2.  An Overview of the Synthesis and Antimicrobial, Antiprotozoal, and Antitumor Activity of Thiazole and Bisthiazole Derivatives.

Authors:  Anca-Maria Borcea; Ioana Ionuț; Ovidiu Crișan; Ovidiu Oniga
Journal:  Molecules       Date:  2021-01-25       Impact factor: 4.411

Review 3.  Marine Cyanobacteria: A Source of Lead Compounds and their Clinically-Relevant Molecular Targets.

Authors:  Lik Tong Tan; Ma Yadanar Phyo
Journal:  Molecules       Date:  2020-05-08       Impact factor: 4.411

Review 4.  Marine Power on Cancer: Drugs, Lead Compounds, and Mechanisms.

Authors:  Lichuan Wu; Ke Ye; Sheng Jiang; Guangbiao Zhou
Journal:  Mar Drugs       Date:  2021-08-27       Impact factor: 5.118

5.  Pharmacodynamic, pharmacokinetic, and phase 1a study of bisthianostat, a novel histone deacetylase inhibitor, for the treatment of relapsed or refractory multiple myeloma.

Authors:  Yu-Bo Zhou; Yang-Ming Zhang; Hong-Hui Huang; Li-Jing Shen; Xiao-Feng Han; Xiao-Bei Hu; Song-da Yu; An-Hui Gao; Li Sheng; Ming-Bo Su; Xiao-Li Wei; Yue Zhang; Yi-Fan Zhang; Zhi-Wei Gao; Xiao-Yan Chen; Fa-Jun Nan; Jia Li; Jian Hou
Journal:  Acta Pharmacol Sin       Date:  2021-08-02       Impact factor: 6.150
  5 in total

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