Article

HIF-1α inhibitors: synthesis and biological evaluation of novel moracin O and P analogues.

College of Pharmacy, Dongguk University-Seoul, Seoul 100-715, South Korea.
European journal of medicinal chemistry (impact factor: 3.27). 06/2011; 46(6):2386-96. DOI:10.1016/j.ejmech.2011.03.022
Source: PubMed

ABSTRACT The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.

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Keywords

2-arylbenzofuran ring
 
benzofuran type moracins
 
cancer cells
 
core scaffold
 
HIF-1α protein accumulation
 
hypoxia
 
hypoxia-inducible factor
 
inhibitory effect
 
key mediator
 
natural products moracins O
 
P exhibited potent
 
R)-configuration
 
representative compound 5
 
structure-activity relationship analysis
 
Systematic variations
 
target gene expression
 
tumour hypoxia
 
vitro inhibitory activity