Synthesis and Structure-Activity Relationship of (E)-Phenoxyacrylic Amide Derivatives as Hypoxia-Inducible Factor (HIF) 1 alpha Inhibitors
- Authors
- Naik, Ravi; Won, Misun; Kim, Bo-Kyung; Xia, Yan; Choi, Hyun Kyung; Jin, Guanghai; Jung, Youngjin; Kim, Hwan Mook; Lee, Kyeong
- Issue Date
- 13-Dec-2012
- Publisher
- AMER CHEMICAL SOC
- Citation
- JOURNAL OF MEDICINAL CHEMISTRY, v.55, no.23, pp.10564 - 10571
- Journal Title
- JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 55
- Number
- 23
- Start Page
- 10564
- End Page
- 10571
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/15931
- DOI
- 10.1021/jm301419d
- ISSN
- 0022-2623
- Abstract
- A series of (E)-phenoxyacrylic amide derivatives were synthesized and evaluated as hypoxia inducible factor (HIF) la inhibitors. The present structure activity relationship study on this series identified the morpholinoethyl containing ester 4p as a potent inhibitor of HIF-1 alpha under hypoxic conditions (IC50 = 0.12 mu M in a cell-based HRE reporter assay) in HCT116 cells. The representative compound 4p suppressed hypoxia-induced HIF-1 alpha accumulation and targeted gene expression in a dose-dependent manner. The effect of HIF-l alpha 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.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - 약학대학 > 약학과 > 1. Journal Articles
![qrcode](https://api.qrserver.com/v1/create-qr-code/?size=55x55&data=https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/15931)
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.