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| Type |
Poster Presentation |
| Area |
Medicinal Chemistry |
| Room No. |
Exhibition Hall 2+3 |
| Time |
10월 19일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-316 |
| Subject |
Synthesis and Biological Evaluation of Phenylsulfonyl Hydrazide Derivatives as Novel mPGES-1 Inhibitors |
| Authors |
sunyoung Kim, Hui Rak Jeong, Jae Yeol Lee*
Department of Chemistry, Kyung Hee University, Korea
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| Abstract |
A novel series of phenylsulfonyl hydrazide derivatives, which were derived from the high throughput screening hit compound 1 (IC50 = 5700 nM against PGE2 production), for a potent inhibitor of mPGES-1 is described. Compound 8n turned out to be most potent lead compound with IC50 value of 4.5 nM and 6.9 nM , respectively, against LPS-1 induced PGE2 and NO production in RAW 264.6 macrophage cells. In addition, 8n was about 30- and > 150-fold more potent against mPGES-1 enzyme in a cell-free assay (IC50 = 70 nM) than MK-886 and hit compound 1, respectively. Molecular docking suggests that compound 8n could inhibit PGE2 production by blocking the PGH2 binding site of human mPGES-1 enzyme. |
| E-mail |
ksy159@khu.ac.kr |
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120th General Meeting of the KCS