Issue 11, 2012
From the journal:

MedChemComm

Synthesis and biological activity of furanylindazoles as inhibitors of hypoxia inducible factor (HIF)-1 transcriptional activity†

Ayano Takeuchi,a   Makihito Hori,a   Shinichi Sato,a   Hyun Seung Ban,a   Takahiro Kuchimaru,b   Shinae Kizaka-Kondoh,b   Takao Yamoric  and  Hiroyuki Nakamura*a  

* Corresponding authors

a Department of Chemistry, Faculty of Science, Gakushuin University, Mejiro, Toshima-ku, Tokyo 171-8588, Japan
E-mail: hiroyuki.nakamura@gakushuin.ac.jp
Fax: +81 359921029
Tel: +81 339860221, ext. 6491

b Department of Biomolecular Engineering, Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology, Yokohama 226-8501, Japan

c Cancer Chemotherapy Center, Japanese Foundation for Cancer Research, Tokyo 170-8455, Japan

Abstract

New YC-1 derivatives were synthesized and evaluated with HIF-1 transcriptional activity, and a potent derivative shows activity in vivo. Furthermore, for the mechanistic study of the YC-1 derivative, we evaluate the antiproliferative activity against 39 human cancer cell lines and the localization of active probes in cells.

Graphical abstract: Synthesis and biological activity of furanylindazoles as inhibitors of hypoxia inducible factor (HIF)-1 transcriptional activity

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Article information

DOI
https://doi.org/10.1039/C2MD20134H
Article type
Concise Article
Submitted
25 May 2012
Accepted
20 Sep 2012
First published
21 Sep 2012

Med. Chem. Commun., 2012,3, 1455-1461

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Synthesis and biological activity of furanylindazoles as inhibitors of hypoxia inducible factor (HIF)-1 transcriptional activity

A. Takeuchi, M. Hori, S. Sato, H. S. Ban, T. Kuchimaru, S. Kizaka-Kondoh, T. Yamori and H. Nakamura, Med. Chem. Commun., 2012, 3, 1455 DOI: 10.1039/C2MD20134H

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