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Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1α inhibitors
- Boovanahalli, Shanthaveerappa K.;
- Jin, Xuejun;
- Jin, Yinglan;
- Kim, Jin Hwan;
- Dat, Nguyen Tien;
- ... Lee, Jeong Hyung;
- 외 4명
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34초록
We report a new series of HIF-1 alpha 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-1 alpha protein in Hep3B cell line, in addition to the dose-dependent inhibition of HIF-1 target genes VEGF and EPO. (C) 2007 Elsevier Ltd. All rights reserved.
키워드
hypoxia; hypoxia-inducible factor; HIF-inhibitor; HIF-1; isonicotinic/nicotinic acid analogues; FACTOR-I; FACTOR 1-ALPHA; HIF; IDENTIFICATION; ANGIOGENESIS; GROWTH; OVEREXPRESSION; EXPRESSION; TARGET
- 제목
- Synthesis of (aryloxyacetylamino)-isonicotinic/nicotinic acid analogues as potent hypoxia-inducible factor (HIF)-1α inhibitors
- 저자
- 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
- 발행일
- 2007-11
- 유형
- Article
- 권
- 17
- 호
- 22
- 페이지
- 6305 ~ 6310