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KMID : 0370220070510050313
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Yakhak Hoeji
2007 Volume.51 No. 5 p.313 ~ p.317
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A New Class of Selective COX-2 Inhibitor: Luotonin A Homologues and their Aza-analogues
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Kim Dong-Hyeon
Jahng Yurng-Dong
Kim Jin-Cheul
Chang Hyun-Wook
Liang Jing-Liu
Oh Joon-Seok
Hong Tae-Gyun
Hwang Nam-Kyung
Chung Hwan-Ki
Kim Yun-Kyung
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Abstract
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A series of luotonin A homologues and their aza-analogues were prepared and evaluated their inhibitory activities on COX-1 and 2 as well as their selectivities on COX-2. The aza-analogue of dimethylene-bridged homologue of luotonin A, 3,3’-dimethylene-2-(1’,8’-naphthyrid-2’-yl)-4(3H)-quinazolinone (2b), exhibited strongest inhibitory activity against COX-1 and COX-2 dependent phase of prostaglandin D_2 generation in mouse bone marrow-derived mast cells in a concentration-dependent manner with an IC_{50} of 39.3 and 1.89{mu}M, respectively. Selectivity of 2b on COX-2 over COX-1 was 21 which implied 2b can be a potential lead for the development of selective COX-2 inhibitor.
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KEYWORD
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luotonin A, COX-2 inhibitor, bone marrow-derived mast cell, prostagladin D_2, 3, 3’-dimethylene-2-(quinolin-2’-yl)-4(3H)-quinazolinone, 3, 3’-dimethylene-2-(1’, 8’-naphthyrid-2’-yl)-4(3H)-quinazolinone
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