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 |
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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)