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Title 

Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as Hypoxia-Inducible Factor (HIF) 1α inhibitors

Authors 

NaikMi Sun WonBo Kyung KimY XiaH K ChoiG JinY JungH M KimK Lee

Publisher 

American Chemical Society

Issue Date 

2012

Citation 

Journal of Medicinal Chemistry, vol. 55, no. 23, pp. 10564-10571

Abstract 

A series of (E)-phenoxyacrylic amide derivatives were synthesized and evaluated as hypoxia inducible factor (HIF) 1α inhibitors. The present structure-activity relationship study on this series identified the morpholinoethyl containing ester 4p as a potent inhibitor of HIF-1α under hypoxic conditions (IC50 = 0.12 μM in a cell-based HRE reporter assay) in HCT116 cells. The representative compound 4p suppressed hypoxia-induced HIF-1α accumulation and targeted gene expression in a dose-dependent manner. The effect of HIF-1α inhibition by 4p was further demonstrated by its inhibitory activity on in vitro tube formation and migration of cells, which may be valuable for development of novel therapeutics for cancer and tumor angiogenesis.

ISSN 

0022-2623

Link 

http://dx.doi.org/10.1021/jm301419d

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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