Literature DB >> 20153643

Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.

Diane H Boschelli1, Joan Subrath, Chuansheng Niu, Biqi Wu, Yan Wang, Julie Lee, Agnes Brennan, Melisa Ho, Bijia Deng, Xiaoke Yang, Xin Xu, Louis Leung, Jianyao Wang, James Atherton, Divya Chaudhary.   

Abstract

Analog 8, a 3-pyridinecarbonitrile with an (E)-2-[6-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]vinyl group at C-5, had an IC(50) value of 1.1 nM for the inhibition of PKCtheta and potently blocked the production of IL-2 in both stimulated murine T cells (IC(50)=34 nM) and human whole blood (IC(50)=500 nM). Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20153643     DOI: 10.1016/j.bmcl.2010.01.119

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


  3 in total

1.  Protein kinase Ctheta is a specific target for inhibition of the HIV type 1 replication in CD4+ T lymphocytes.

Authors:  María Rosa López-Huertas; Elena Mateos; Gema Díaz-Gil; Francisco Gómez-Esquer; María Sánchez del Cojo; José Alcamí; Mayte Coiras
Journal:  J Biol Chem       Date:  2011-06-13       Impact factor: 5.157

Review 2.  The Novel PKCθ from Benchtop to Clinic.

Authors:  Rouba Hage-Sleiman; Asmaa B Hamze; Lina Reslan; Hadile Kobeissy; Ghassan Dbaibo
Journal:  J Immunol Res       Date:  2015-05-19       Impact factor: 4.818

3.  Pharmacological Inhibition of PKCθ Counteracts Muscle Disease in a Mouse Model of Duchenne Muscular Dystrophy.

Authors:  V Marrocco; P Fiore; A Benedetti; S Pisu; E Rizzuto; A Musarò; L Madaro; B Lozanoska-Ochser; M Bouché
Journal:  EBioMedicine       Date:  2017-01-07       Impact factor: 8.143

  3 in total

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