Literature DB >> 12182863

Structure-activity relationship studies of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine-5-carboxylate: an inhibitor of AP-1 and NF-kappaB mediated gene expression.

Moorthy S S Palanki1, Leah M Gayo-Fung, Graziella I Shevlin, Paul Erdman, Mark Sato, Mark Goldman, Lynn J Ransone, Cheryl Spooner.   

Abstract

Several analogues of ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))amino]-4-(trifluoromethyl)pyrimidine-5-carboxylate (1) were synthesized and tested as inhibitors of AP-1 and NF-kappaB mediated transcriptional activation in Jurkat T cells. From our SAR work, ethyl 2-[(3-methyl-2,5-dioxo(3-pyrrolinyl))-N-methylamino]-4-(trifluoromethyl)-pyrimidine-5-carboxylate was identified as a novel and potent inhibitor.

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Year:  2002        PMID： 12182863     DOI： 10.1016/s0960-894x(02)00517-6

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


  9 in total

1.  Theoretical studies on pyrimidine substituent derivatives as dual inhibitors of AP-1 and NF-kappaB.

Authors:  Li Qian; Si-Yan Liao; Zu-Liang Huang; Yong Shen; Kang-Cheng Zheng
Journal:  J Mol Model       Date:  2009-11-27       Impact factor: 1.810

2.  Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors.

Authors:  Michele Ceribelli; Priscilla N Kelly; Arthur L Shaffer; George W Wright; Wenming Xiao; Yibin Yang; Lesley A Mathews Griner; Rajarshi Guha; Paul Shinn; Jonathan M Keller; Dongbo Liu; Paresma R Patel; Marc Ferrer; Shivangi Joshi; Sujata Nerle; Peter Sandy; Emmanuel Normant; Craig J Thomas; Louis M Staudt
Journal:  Proc Natl Acad Sci U S A       Date:  2014-07-21       Impact factor: 11.205

Review 3.  Research developments in the syntheses, anti-inflammatory activities and structure-activity relationships of pyrimidines.

Authors:  Haroon Ur Rashid; Marco Antonio Utrera Martines; Adriana Pereira Duarte; Juliana Jorge; Shagufta Rasool; Riaz Muhammad; Nasir Ahmad; Muhammad Naveed Umar
Journal:  RSC Adv       Date:  2021-02-03       Impact factor: 3.361

Review 4.  Advances in targeting IKK and IKK-related kinases for cancer therapy.

Authors:  Dung-Fang Lee; Mien-Chie Hung
Journal:  Clin Cancer Res       Date:  2008-09-15       Impact factor: 12.531

Review 5.  Chronic inflammation and cancer: potential chemoprevention through nuclear factor kappa B and p53 mutual antagonism.

Authors:  Srabani Pal; Ashish Bhattacharjee; Asif Ali; Narayan C Mandal; Subhash C Mandal; Mahadeb Pal
Journal:  J Inflamm (Lond)       Date:  2014-08-09       Impact factor: 4.981

6.  Mutation of cysteine 46 in IKK-beta increases inflammatory responses.

Authors:  Ting Li; Vincent Kam Wai Wong; Zhi Hong Jiang; Shui Ping Jiang; Yan Liu; Ting Yu Wang; Xiao Jun Yao; Xiao Hui Su; Feng Gen Yan; Juan Liu; Elaine Lai-Han Leung; Xiao Qin Yi; Yuen Fan Wong; Hua Zhou; Liang Liu
Journal:  Oncotarget       Date:  2015-10-13

7.  Small molecule inhibitors targeting activator protein 1 (AP-1).

Authors:  Na Ye; Ye Ding; Christopher Wild; Qiang Shen; Jia Zhou
Journal:  J Med Chem       Date:  2014-05-27       Impact factor: 8.039

Review 8.  Targeting IKKβ in Cancer: Challenges and Opportunities for the Therapeutic Utilisation of IKKβ Inhibitors.

Authors:  Jack A Prescott; Simon J Cook
Journal:  Cells       Date:  2018-08-23       Impact factor: 6.600

Review 9.  Synthetic approaches and pharmacological activity of 1,3,4-oxadiazoles: a review of the literature from 2000-2012.

Authors:  Cledualdo Soares de Oliveira; Bruno Freitas Lira; José Maria Barbosa-Filho; Jorge Gonçalo Fernandez Lorenzo; Petrônio Filgueiras de Athayde-Filho
Journal:  Molecules       Date:  2012-08-27       Impact factor: 4.411
  9 in total

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