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

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Title
Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1α inhibitors
Author(s)
S K Boovanahalli; X Jin; Y Jin; J H Kim; N T Dat; Young-Soo Hong; J H Lee; S H Jung; Kyeong Lee; Jung Joon Lee
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 17, no. 12, pp. 6305-6310
Publication Year
2007
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.
Keyword
HIF-1HIF-inhibitorhypoxiahypoxia-inducible factorisonicotinic/nicotinic acid analogues
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2007.09.005
Type
Article
Appears in Collections:
Ochang Branch Institute > Anticancer Agent Research Center > 1. Journal Articles
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