Diaryl-substituted carboranes as inhibitors of hypoxia inducible factor-1 transcriptional activity

Hiroyuki Nakamura, Lisa Tazaki, Daisuke Kanoh, Shinichi Sato

Research output: Contribution to journalArticlepeer-review

6 Citations (Scopus)


Diaryl-substituted carboranes, as a new class of HIF-1α inhibitors, were synthesized from the corresponding diaryl-substituted alkynes by decaborane coupling. The microwave-irradiated conditions with a combination of N,N-dimethylaniline and chlorobenzene were effective to obtain the diaryl-substituted carboranes in good to high yields. Among the compounds synthesized, compounds 1a and 1d showed significant inhibition of HIF-1 mediated transcriptional activity under hypoxia. Both compounds similarly suppressed hypoxia-induced HIF-1α accumulation in a concentration-dependent manner without affecting HIF-1α mRNA expression.

Original languageEnglish
Pages (from-to)143-154
Number of pages12
JournalPure and Applied Chemistry
Issue number2
Publication statusPublished - 2015 Feb 1
Externally publishedYes


  • Cancer therapy
  • Diaryl-substituted carboranes
  • Hypoxia inducible factor-1 (HIF-1)

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)


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