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.
| Original language | English |
|---|---|
| Pages (from-to) | 143-154 |
| Number of pages | 12 |
| Journal | Pure and Applied Chemistry |
| Volume | 87 |
| Issue number | 2 |
| DOIs | |
| Publication status | Published - 2015 Feb 1 |
| Externally published | Yes |
Keywords
- Cancer therapy
- Diaryl-substituted carboranes
- Hypoxia inducible factor-1 (HIF-1)
- IMEBORON XV
ASJC Scopus subject areas
- Chemistry(all)
- Chemical Engineering(all)
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Nakamura, H., Tazaki, L., Kanoh, D., & Sato, S. (2015). Diaryl-substituted carboranes as inhibitors of hypoxia inducible factor-1 transcriptional activity. Pure and Applied Chemistry, 87(2), 143-154. https://doi.org/10.1515/pac-2014-0911