TY - JOUR
T1 - Synthesis and biological evaluation of meta-carborane-containing phenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity
AU - Li, Guangzhe
AU - Azuma, Soyoko
AU - Minegishi, Hidemitsu
AU - Nakamura, Hiroyuki
PY - 2015/3/30
Y1 - 2015/3/30
N2 - meta-Carboranylphenoxyacetanilides were synthesized by copper catalyzed coupling reaction of meta-carborane and phenyl iodides. The synthesized compounds were evaluated for their ability to inhibit hypoxia-induced HIF-1 transcriptional activity using a cell-based reporter gene assay. Among the compounds synthesized, meta-carborane containing phenoxyanilides 2d and 2h, which have an isobutyl group on meta-carborane, exhibited significant inhibition of hypoxia-induced HIF-1 transcriptional activity toward HeLa cell-based reporter gene assay with the IC50 values of 0.73 and 0.55μM, respectively.
AB - meta-Carboranylphenoxyacetanilides were synthesized by copper catalyzed coupling reaction of meta-carborane and phenyl iodides. The synthesized compounds were evaluated for their ability to inhibit hypoxia-induced HIF-1 transcriptional activity using a cell-based reporter gene assay. Among the compounds synthesized, meta-carborane containing phenoxyanilides 2d and 2h, which have an isobutyl group on meta-carborane, exhibited significant inhibition of hypoxia-induced HIF-1 transcriptional activity toward HeLa cell-based reporter gene assay with the IC50 values of 0.73 and 0.55μM, respectively.
KW - Hypoxia inducible factor
KW - Inhibitor
KW - meta-Carborane
KW - Transcription
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U2 - 10.1016/j.jorganchem.2015.05.029
DO - 10.1016/j.jorganchem.2015.05.029
M3 - Article
SN - 0022-328X
JO - Journal of Organometallic Chemistry
JF - Journal of Organometallic Chemistry
ER -