Design, synthesis, and structure-activity relationship study of halogen containing 2-benzylidene-1-indanone derivatives for inhibition of LPS-stimulated ROS production in RAW 264.7 macrophagesRAW 264.7 대식세포에서 halogen containing 2-benzylidene-1-indanone 파생물의 설계, 합성, 구조활성 관계가 항산화에 미치는 연구
- Other Titles
- RAW 264.7 대식세포에서 halogen containing 2-benzylidene-1-indanone 파생물의 설계, 합성, 구조활성 관계가 항산화에 미치는 연구
- Authors
- Shrestha A.; Jin Oh H.; Kim M.J.; Pun N.T.; Magar T.B.T.; Bist G.; Choi H.; Park P.-H.; Lee E.-S.
- Issue Date
- Jun-2017
- Publisher
- Elsevier Masson SAS62 rue Camille DesmoulinsIssy les Moulineaux Cedex92442
- Citation
- European Journal of Medicinal Chemistry, v.133, pp.121 - 138
- Journal Title
- European Journal of Medicinal Chemistry
- Volume
- 133
- Start Page
- 121
- End Page
- 138
- URI
- http://scholarworks.bwise.kr/kbri/handle/2023.sw.kbri/943
- ISSN
- 0223-5234
- Abstract
- As a continuous effort to discover new potential anti-inflammatory agents, we systematically designed and synthesized sixty-one 2-benzylidene-1-indanone derivatives with structural modification of chalcone, and evaluated their inhibitory activity on LPS-stimulated ROS production in RAW 264.7 macrophages. Systematic structure-activity relationship study revealed that hydroxyl group in C-5, C-6, or C-7 position of indanone moiety, and ortho-, meta-, or para-fluorine, trifluoromethyl, trifluoromethoxy, and bromine functionalities in phenyl ring are important for inhibition of ROS production in LPS-stimulated RAW 264.7 macrophages. Among all the tested compounds, 6-hydroxy-2-(2-(trifluoromethoxy) benzylidene)-2,3-dihydro-1H-inden-1-one (compound 44) showed the strongest inhibitory activity of ROS production. Further studies on the mode of action revealed that compound 44 potently suppressed LPS-stimulated ROS production via modulation of NADPH oxidase. The findings of this work could be useful to design 2-benzylidene-indanone based lead compounds as novel anti-inflammatory agents.
- Files in This Item
- There are no files associated with this item.
- Appears in
Collections - ETC > 1. Journal Articles
![qrcode](https://api.qrserver.com/v1/create-qr-code/?size=55x55&data=http://scholarworks.bwise.kr/kbri/handle/2023.sw.kbri/943)
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.