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

SK Boovanahalli, X Jin, Y Jin, JH Kim, NT Dat…

Index: Boovanahalli, Shanthaveerappa K.; Jin, Xuejun; Jin, Yinglan; Kim, Jin Hwan; Dat, Nguyen Tien; Hong, Young-Soo; Lee, Jeong Hyung; Jung, Sang-Hun; Lee, Kyeong; Lee, Jung Joon Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 22 p. 6305 - 6310

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Citation Number: 25

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 ...