Literature DB >> 23538115

Discovery of adamantane based highly potent HDAC inhibitors.

Balasubramanian Gopalan1, Thanasekaran Ponpandian, Virendra Kachhadia, Kuppusamy Bharathimohan, Radhakrishnan Vignesh, Velaiah Sivasudar, Shridhar Narayanan, Bhonde Mandar, Rajendran Praveen, Nithyanandan Saranya, Sriram Rajagopal, Sridharan Rajagopal.   

Abstract

Herein, we report the development of highly potent HDAC inhibitors for the treatment of cancer. A series of adamantane and nor-adamantane based HDAC inhibitors were designed, synthesized and screened for the inhibitory activity of HDAC. A number of compounds exhibited GI50 of 10-100 nM in human HCT116, NCI-H460 and U251 cancer cells, in vitro. Compound 32 displays efficacy in human tumour animal xenograft model.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23538115     DOI: 10.1016/j.bmcl.2013.03.002

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  New and emerging HDAC inhibitors for cancer treatment.

Authors:  Alison C West; Ricky W Johnstone
Journal:  J Clin Invest       Date:  2014-01-02       Impact factor: 14.808

2.  Novel hydroxamates potentiated in vitro activity of fluconazole against Candida albicans.

Authors:  Maneesh Paul-Satyaseela; Periasamy Hariharan; Thirunavukkarasu Bharani; Jonathan S Franklyne; Thangapazham Selvakumar; Kuppusamy Bharathimohan; Chenniappan Vinoth Kumar; Virendra Kachhadia; Shridhar Narayanan; Sridharan Rajagopal; Gopalan Balasubramanian
Journal:  J Nat Sci Biol Med       Date:  2017 Jan-Jun

Review 3.  Molecular Imaging of Hydrolytic Enzymes Using PET and SPECT.

Authors:  Brian P Rempel; Eric W Price; Christopher P Phenix
Journal:  Mol Imaging       Date:  2017 Jan-Dec       Impact factor: 4.488

4.  In vivo imaging of histone deacetylases (HDACs) in the central nervous system and major peripheral organs.

Authors:  Changning Wang; Frederick A Schroeder; Hsiao-Ying Wey; Ronald Borra; Florence F Wagner; Surya Reis; Sung Won Kim; Edward B Holson; Stephen J Haggarty; Jacob M Hooker
Journal:  J Med Chem       Date:  2014-09-18       Impact factor: 7.446

Review 5.  Advances in the Development of PET Ligands Targeting Histone Deacetylases for the Assessment of Neurodegenerative Diseases.

Authors:  Tetsuro Tago; Jun Toyohara
Journal:  Molecules       Date:  2018-01-31       Impact factor: 4.411

  5 in total

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