Diaryl-substituted ortho-carboranes as a new class of hypoxia inducible factor-1alpha inhibitors.

Article Details

Citation

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.