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Title
Japanese:Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors 
English:Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors 
Author
Japanese: Hidemitsu Minegishi, Shinji Fukashiro, Hyun Seung Ban, Hiroyuki Nakamura.  
English: Hidemitsu Minegishi, Shinji Fukashiro, Hyun Seung Ban, Hiroyuki Nakamura.  
Language English 
Journal/Book name
Japanese:ACS Medicinal Chemistry Letters 
English:ACS Medicinal Chemistry Letters 
Volume, Number, Page Vol. 4        pp. 297-301
Published date Jan. 27, 2013 
Publisher
Japanese: 
English: 
Conference name
Japanese: 
English: 
Conference site
Japanese: 
English: 
Official URL http://dx.doi.org/10.1021/ml3004632
 
DOI https://doi.org/10.1021/ml3004632
Abstract The indenopyrazole framework was investigated as a new class of HIF-1α inhibitors. Indenopyrazole 2l was found to most strongly inhibit the hypoxia-induced HIF-1α transcriptional activity (IC50 = 0.014 μM) among all of the known compounds having relatively simple structures, unlike manassantins. Indenopyrazole 2l suppressed HIF-1α transcriptional activity without affecting both HIF-1α protein accumulation and HIF-1α/HIF-1β heterodimerization in nuclei under the hypoxic conditions, suggesting that 2l probably affected the transcriptional pathway induced by the HIF-1α/HIF-1β heterodimer.

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