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Title 

Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1α inhibitors

Authors 

S K BoovanahalliX JinY JinJ H KimN T DatYoung-Soo HongJ H LeeS H JungKyeong LeeJung Joon Lee

Publisher 

Elsevier

Issue Date 

2007

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 17, no. 12, pp. 6305-6310

Keywords 

HIF-1HIF-inhibitorhypoxiahypoxia-inducible factorisonicotinic/nicotinic acid analoguesacetic acid derivativehypoxia inducible factor 1alphaisonicotinic acidnicotinic acid derivativedrug synthesis

Abstract 

We report a new series of HIF-1α inhibitors which were obtained through structural modifications of previously reported lead 1. The in vitro inhibitory potencies of newly synthesized compounds were evaluated against hypoxia-induced HIF-1 activation using cell-based reporter assay in three human cancer cell lines including SK-Hep-1, Hep3B, and AGS cells. Several compounds displayed significant inhibitory activity in all the three tested cell lines. In particular, analogue 17 displayed potent inhibition of hypoxia-induced accumulation of HIF-1α protein in Hep3B cell line, in addition to the dose-dependent inhibition of HIF-1 target genes VEGF and EPO.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2007.09.005

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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