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Discovery and structure–activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors

Noguchi-Yachide, Tomomi ; Sakai, Taki ; Hashimoto, Yuichi ; Yamaguchi, Takao

Bioorganic & Medicinal Chemistry, 01 March 2015, Vol.23(5), pp.953-959 [Peer Reviewed Journal]

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  • Title:
    Discovery and structure–activity relationship studies of N6-benzoyladenine derivatives as novel BRD4 inhibitors
  • Author: Noguchi-Yachide, Tomomi ; Sakai, Taki ; Hashimoto, Yuichi ; Yamaguchi, Takao
  • Description: Bromodomain and extra-terminal domain (BET) proteins are epigenetic readers that bind to acetylated lysines in histones. Among them, BRD4 is a candidate target molecule of therapeutic agents for diverse diseases, including cancer and inflammatory disease. As a part of our continuing structural development studies of thalidomide to obtain a broad spectrum of biological modifiers based on the ‘multi-template’ approach, in this work we focused on BRD4-inhibitory activity, and discovered that 6-benzoyladenine derivatives exhibit this activity. Structure–activity relationship studies led to 6-(2,4,5-trimethoxybenzoyl)adenine ( ), which exhibits potent BRD4 bromodomain1 inhibitory activity with an IC value of 0.427 μM. 6-Benzoyladenine appears to be a new chemical scaffold for development of BRD4 inhibitors.
  • Is Part Of: Bioorganic & Medicinal Chemistry, 01 March 2015, Vol.23(5), pp.953-959
  • Identifier: ISSN: 0968-0896 ; E-ISSN: 1464-3391 ; DOI: 10.1016/j.bmc.2015.01.022
  • Subjects: Brd4 ; Bromodomain ; Benzoyladenine ; Structure–Activity Relationship ; Medicine ; Chemistry ; Anatomy & Physiology
  • Language: English

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