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- Title
Diaryl-substituted carboranes as inhibitors of hypoxia inducible factor-1 transcriptional activity.
- Authors
Nakamura, Hiroyuki; Tazaki, Lisa; Kanoh, Daisuke; Sato, Shinichi
- 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.
- Subjects
CARBORANES; HYPOXIA-inducible factor 1; ALKYNES; GENE regulatory networks; MESSENGER RNA
- Publication
Pure & Applied Chemistry, 2015, Vol 87, Issue 2, p143
- ISSN
0033-4545
- Publication type
Article
- DOI
10.1515/pac-2014-0911