TY - JOUR
T1 - Ortho-Carboranylphenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity and heat shock protein (HSP) 60 chaperon activity
AU - Li, Guangzhe
AU - Azuma, Soyoko
AU - Sato, Shinichi
AU - Minegishi, Hidemitsu
AU - Nakamura, Hiroyuki
N1 - Funding Information:
This work was partially supported by a Grant-in-Aid for Scientific Research on Innovative Areas ‘Chemical Biology of Natural Products’ from The Ministry of Education, Culture, Sports, Science and Technology, Japan .
Publisher Copyright:
© 2015 Elsevier Ltd. All rights reserved.
PY - 2015/5/30
Y1 - 2015/5/30
N2 - ortho-Carboranylphenoxy derivatives were synthesized and evaluated for their ability to inhibit hypoxia-induced HIF-1 transcriptional activity using a cell-based reporter gene assay. Among the compounds synthesized, compound 1d showed the most significant inhibition of hypoxia-induced HIF-1 transcriptional activity with the IC50 of 0.53 μM. Furthermore, compound 1h was found to possess the most significant inhibition of heat shock protein (HSP) 60 chaperon activity among the reported inhibitors: the IC50 toward the porcine heart malate dehydrogenase (MDH) refolding assay was 0.35 μM.
AB - ortho-Carboranylphenoxy derivatives were synthesized and evaluated for their ability to inhibit hypoxia-induced HIF-1 transcriptional activity using a cell-based reporter gene assay. Among the compounds synthesized, compound 1d showed the most significant inhibition of hypoxia-induced HIF-1 transcriptional activity with the IC50 of 0.53 μM. Furthermore, compound 1h was found to possess the most significant inhibition of heat shock protein (HSP) 60 chaperon activity among the reported inhibitors: the IC50 toward the porcine heart malate dehydrogenase (MDH) refolding assay was 0.35 μM.
KW - Angiogenesis
KW - Carborane
KW - Heat shock protein (HSP) 60
KW - Hypoxia-inducible factor (HIF)-1α
KW - Inhibitor
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U2 - 10.1016/j.bmcl.2015.04.088
DO - 10.1016/j.bmcl.2015.04.088
M3 - Article
C2 - 25981686
AN - SCOPUS:84930091269
VL - 25
SP - 2624
EP - 2628
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
SN - 0960-894X
IS - 13
ER -