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Title
Japanese:Diaryl-substituted carboranes as inhibitors of hypoxia inducible factor-1 transcriptional activity 
English:Diaryl-substituted carboranes as inhibitors of hypoxia inducible factor-1 transcriptional activity 
Author
Japanese: 中村 浩之, Lisa Tazaki, Daisuke Kanoh, 佐藤 伸一.  
English: Hiroyuki Nakamura, Lisa Tazaki, Daisuke Kanoh, Shinichi Sato.  
Language English 
Journal/Book name
Japanese:Pure and Applied Chemistry 
English:Pure and Applied Chemistry 
Volume, Number, Page Vol. 87    No. 2    pp. 143-154
Published date Feb. 2015 
Publisher
Japanese: 
English: 
Conference name
Japanese: 
English: 
Conference site
Japanese: 
English: 
DOI https://doi.org/10.1039/c3dt52828f
Abstract 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.

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