EventsThe 12th International Electronic Conference on Synthetic Organic Chemistry
Published
This submission belongs to the session c. Bioorganic Chemistry and Natural Products of the event The 12th International Electronic Conference on Synthetic Organic Chemistry
Published date
20 Nov, 2008
Citation
Thanh-Dao Tran, Haeil Park, Gerhard F. Ecker, Khac-Minh Thai, 2’-Hydroxychalcone Analogues: Synthesis and Structure-PGE2 Inhibitory Activity Relationship, in Proceedings of The 12th International Electronic Conference on Synthetic Organic Chemistry, 1 November–30 November 2008, MDPI: Basel, Switzerland, doi: 10.3390/ecsoc-12-01247
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2’-Hydroxychalcone Analogues: Synthesis and Structure-PGE2 Inhibitory Activity Relationship

Haeil Park 2
Gerhard F. Ecker 3
Khac-Minh Thai 1,3
1. Department of Pharmaceutical Chemistry, University of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang, Dist. 1, Ho Chi Minh City, Vietnam
2. College of Pharmacy, Kangwon National University, Chuncheon 200-701, Republic of Korea
3. Emerging Field Pharmacoinformatics, Department of Medicinal Chemistry, University of Vienna, Althanstrasse 14, A-1090, Vienna, Austria
Abstract
A series of 2’-hydroxychalcones was synthesized and screened for their in vitro inhibitory effects on PGE2 production from RAW 264.7 cells induced by LPS. Structure–activity relationship study suggested that inhibitory activity of PGE2 formation was governed to a greater extent by the substituent on B ring of the chalcone template, and most of the active compounds have at least two methoxyl or benzyloxyl groups on B ring. The relationship between chalcone structures and their PGE2 inhibitory activity was also interpreted by docking study on cyclooxygenase 2.
Keywords
n/a
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