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

Hiroyuki Nakamura, Lisa Tazaki, Daisuke Kanoh, Shinichi Sato

研究成果: Article

5 引用 (Scopus)

抜粋

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.

元の言語English
ページ(範囲)143-154
ページ数12
ジャーナルPure and Applied Chemistry
87
発行部数2
DOI
出版物ステータスPublished - 2015 2 1
外部発表Yes

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

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