Diaryl-substituted ortho-carboranes as a new class of hypoxia inducible factor-1α inhibitors?

Dalton Transactions Pub Date: 2013-11-19 DOI: 10.1039/C3DT52828F

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-1α accumulation in a concentration-dependent manner without affecting HIF-1α mRNA expression.

Graphical abstract: Diaryl-substituted ortho-carboranes as a new class of hypoxia inducible factor-1α inhibitors
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