Synthesis and biological evaluation of meta-carborane-containing phenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity

Guangzhe Li, Soyoko Azuma, Hidemitsu Minegishi, Hiroyuki Nakamura

Research output: Contribution to journalArticlepeer-review

11 Citations (Scopus)

Abstract

meta-Carboranylphenoxyacetanilides were synthesized by copper catalyzed coupling reaction of meta-carborane and phenyl iodides. The synthesized compounds were evaluated for their ability to inhibit hypoxia-induced HIF-1 transcriptional activity using a cell-based reporter gene assay. Among the compounds synthesized, meta-carborane containing phenoxyanilides 2d and 2h, which have an isobutyl group on meta-carborane, exhibited significant inhibition of hypoxia-induced HIF-1 transcriptional activity toward HeLa cell-based reporter gene assay with the IC<inf>50</inf> values of 0.73 and 0.55μM, respectively.

Original languageEnglish
JournalJournal of Organometallic Chemistry
DOIs
Publication statusAccepted/In press - 2015 Mar 30

Keywords

  • Hypoxia inducible factor
  • Inhibitor
  • meta-Carborane
  • Transcription

ASJC Scopus subject areas

  • Inorganic Chemistry
  • Organic Chemistry
  • Physical and Theoretical Chemistry
  • Materials Chemistry
  • Biochemistry

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