Ortho-Carboranylphenoxyacetanilides as inhibitors of hypoxia-inducible factor (HIF)-1 transcriptional activity and heat shock protein (HSP) 60 chaperon activity

Guangzhe Li, Soyoko Azuma, Shinichi Sato, Hidemitsu Minegishi, Hiroyuki Nakamura

Research output: Contribution to journalArticlepeer-review

13 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)2624-2628
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number13
DOIs
Publication statusPublished - 2015 May 30

Keywords

  • Angiogenesis
  • Carborane
  • Heat shock protein (HSP) 60
  • Hypoxia-inducible factor (HIF)-1α
  • Inhibitor

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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