Diaryl-substituted ortho-carboranes as a new class of hypoxia inducible factor-1alpha inhibitors.
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Nakamura H, Tasaki L, Kanoh D, Sato S, Ban HS
Diaryl-substituted ortho-carboranes as a new class of hypoxia inducible factor-1alpha inhibitors.
Dalton Trans. 2014 Apr 7;43(13):4941-4. doi: 10.1039/c3dt52828f.
- PubMed ID
- 24270971 [ View in PubMed]
- Abstract
Diaryl-substituted ortho-carboranes 1 were synthesized from the corresponding alkynes by decaborane coupling under microwave-irradiated conditions with a combination of N,N-dimethylaniline and chlorobenzene. Among the compounds synthesized, 1a and 1d exhibited significant inhibition of hypoxia-induced HIF-1 transcriptional activity. Both compounds similarly suppressed hypoxia-induced HIF-1alpha accumulation in a concentration-dependent manner without affecting HIF-1alpha mRNA expression.